nur für Forschungszwecke
Dasatinib Monohydrate Src Inhibitor
Kat.-Nr.S7782
Chemische Struktur
Molekulargewicht: 506.02
Springe zu
Qualitätskontrolle
Charge:
Reinheit:
99.62%
99.62
| Verwandte Ziele | EGFR VEGFR JAK PDGFR FGFR HIF FLT FLT3 HER2 Bcr-Abl |
|---|---|
| Weitere Src Inhibitoren | WH-4-023 Saracatinib (AZD0530) PP2 (AGL 1879) SU6656 PP1 Src Inhibitor 1 Tolimidone (MLR-1023) UM-164 1-Naphthyl PP1(1-NA-PP1) RK 24466 |
Zellkultur, Behandlung & Arbeitskonzentration
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| K562 cell | Proliferation assay | 72 h | Antiproliferative activity against human K562 cells after 72 hrs, IC50=0.001 μM | |||
| WiDr cell | Proliferation assay | 72 h | Antiproliferative activity against human WiDr cells after 72 hrs, IC50=0.052 μM | |||
| PC3 cell | Proliferation assay | 72 h | Antiproliferative activity against human PC3 cells after 72 hrs, IC50=0.0094 μM | |||
| MDA-MB-231 cell | Proliferation assay | 72 h | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs, IC50=0.012 μM | |||
| M07ep210 cell | Growth inhibition assay | 48 h | Growth inhibition of human M07ep210 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.07 nM | |||
| K562 cell | Growth inhibition assay | 48 h | Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.001 μM | |||
| M07e cell | Growth inhibition assay | 48 h | Growth inhibition of human M07e cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.0012 μM | |||
| K562 cell | Cytotoxicity assay | 72 h | Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=12.83 μM | |||
| U937 cell | Cytotoxicity assay | 72 h | Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=13.63 μM | |||
| K562 cell | Proliferation assay | 72 h | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50=0.7 nM | |||
| MDA-MB-435S cell | Proliferation assay | 72 h | Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50=3.9 μM | |||
| NCI-H460 cell | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50=8.99 μM | |||
| NCI-H23 cell | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50=2.27 μM | |||
| A549 cell | Proliferation assay | 72 h | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=12.66 μM | |||
| T47D cell | Proliferation assay | 72 h | Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50=0.9 μM | |||
| HCT116 cell | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.3 μM | |||
| MCF7 cells | Proliferation assay | 72 h | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=2.57 μM | |||
| RXF 393NL cell | Cytotoxicity assay | 4 days | Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining, IC50=21.7 nM | |||
| PRXF DU145 cell | Cytotoxicity assay | 4 days | Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining, IC50=0.0623 μM | |||
| LXFA 983L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human LXFA 983L cells after 4 days by propidium iodide staining, IC50=56.5 nM | |||
| GXF251L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining, IC50=2.25 μM | |||
| CXF 1103L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human CXF 1103L cells after 4 days by propidium iodide staining, IC50=4.36 μM | |||
| PAXF 1657L cell | Cytotoxicity assay | 4 days | Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining, IC50=0.121 μM | |||
| NCI-H1648 cell | Growth inhibition assay | Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.02011 μM | ||||
| NCI-H1838 cell | Growth inhibition assay | Inhibition of human NCI-H1838 cell growth in a cell viability assay, IC50=1.30733 μM | ||||
| NCI-H2126 cell | Growth inhibition assay | Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=2.87552 μM | ||||
| NCI-H2141 cell | Growth inhibition assay | Inhibition of human NCI-H2141 cell growth in a cell viability assay, IC50=24.7754 μM | ||||
| NCI-H2107 cell | Growth inhibition assay | Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=43.4847 μM | ||||
| NCI-H747 cell | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.08362 μM | ||||
| NCI-H720 cell | Growth inhibition assay | Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=20.2733 μM | ||||
| NKM-1 cell | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay.IC50=1.30859 μM | ||||
| NMC-G1 cell | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay.IC50=0.11606 μM | ||||
| NTERA-S-cl-D1 cell | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.IC50=0.12283 μM | ||||
| OCI-AML2 cell | Growth inhibition assay | Inhibition of human OCI-AML2 cell growth in a cell viability assay.IC50=5.86154 μM | ||||
| OCUB-M cell | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay.IC50=1.04412 μM | ||||
| OPM-2 cell | Growth inhibition assay | Inhibition of human OPM-2 cell growth in a cell viability assay.IC50=4.27685 μM | ||||
| OS-RC-2 cell | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay.IC50=0.0203 μM | ||||
| ONS-76 cell | Growth inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay.IC50=0.42951 μM | ||||
| OVCAR-4 cell | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay.IC50=0.37433 μM | ||||
| NCI-H446 cell | Growth inhibition assay | Inhibition of human NCI-H446 cell growth in a cell viability assay.IC50=0.6276 μM | ||||
| NCI-H510A cell | Growth inhibition assay | Inhibition of human NCI-H510A cell growth in a cell viability assay.IC50=19.3973 μM | ||||
| PF-382 cell | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay.IC50=0.17678 μM | ||||
| NCI-H64 cell | Growth inhibition assay | Inhibition of human NCI-H64 cell growth in a cell viability assay.IC50=29.6253 μM | ||||
| PSN1 cell | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay.IC50=0.04474 μM | ||||
| QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay.IC50=0.70629 μM | ||||
| RL95-2 cell | Growth inhibition assay | Inhibition of human RL95-2 cell growth in a cell viability assay.IC50=0.1038 μM | ||||
| RCC10RGB cell | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay.IC50=0.4911 μM | ||||
| RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay.IC50=0.52966 μM | ||||
| NCI-SNU-16 cell | Growth inhibition assay | Inhibition of human NCI-SNU-16 cell growth in a cell viability assay.IC50=8.56128 μM | ||||
| RPMI-6666 cell | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay.IC50=7.27067 μM | ||||
| NEC8 cell | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay.IC50=44.336 μM | ||||
| RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay.IC50=7.65787 μM | ||||
| RXF393 cell | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay.IC50=0.02357 μM | ||||
| Raji cell | Growth inhibition assay | Inhibition of human Raji cell growth in a cell viability assay.IC50=13.7497 μM | ||||
| NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay.IC50=0.006129 μM | ||||
| SBC-1 cell | Growth inhibition assay | Inhibition of human SBC-1 cell growth in a cell viability assay.IC50=1.57984 μM | ||||
| SF126 cell | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay.IC50=0.3541 μM | ||||
| SF539 cell | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay.IC50=13.8557 μM | ||||
| SH-4 cell | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay.IC50=0.18413 μM | ||||
| OMC-1 cell | Growth inhibition assay | Inhibition of human OMC-1 cell growth in a cell viability assay.IC50=27.1422 μM | ||||
| SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay.IC50=9.02493 μM | ||||
| SJSA-1 cell | Growth inhibition assay | Inhibition of human SJSA-1 cell growth in a cell viability assay.IC50=8.72805 μM | ||||
| SK-LMS-1 cell | Growth inhibition assay | Inhibition of human SK-LMS-1 cell growth in a cell viability assay.IC50=3.11886 μM | ||||
| SK-NEP-1 cell | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay.IC50=8.89155 μM | ||||
| SKM-1 cell | Growth inhibition assay | Inhibition of human SKM-1 cell growth in a cell viability assay.IC50=9.01734 μM | ||||
| SK-PN-DW cell | Growth inhibition assay | Inhibition of human SK-PN-DW cell growth in a cell viability assay.IC50=36.1943 μM | ||||
| SK-UT-1 cell | Growth inhibition assay | Inhibition of human SK-UT-1 cell growth in a cell viability assay.IC50=2.16693 μM | ||||
| SNB75 cell | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay.IC50=0.04435 μM | ||||
| REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay.IC50=20.6357 μM | ||||
| SNU-C2B cell | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay.IC50=1.30589 μM | ||||
| RPMI-8866 cell | Growth inhibition assay | Inhibition of human RPMI-8866 cell growth in a cell viability assay.IC50=17.4455 μM | ||||
| SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay.IC50=0.04161 μM | ||||
| SW962 cell | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay.IC50=0.11292 μM | ||||
| SF268 cell | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay.IC50=0.17404 μM | ||||
| TE-1 cell | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay.IC50=0.1054 μM | ||||
| 8-MG-BA cell | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay.IC50=0.15458 μM | ||||
| A101D cell | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay.IC50=1.03043 μM | ||||
| A253 cell | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay.IC50=3.73246 μM | ||||
| A3-KAW cell | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay.IC50=0.98452 μM | ||||
| A4-Fuk cell | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay.IC50=38.1009 μM | ||||
| A388 cell | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay.IC50=0.05095 μM | ||||
| ACN cell | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay.IC50=1.82252 μM | ||||
| A704 cell | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay.IC50=0.01491 μM | ||||
| ALL-PO cell | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay.IC50=10.7938 μM | ||||
| ARH-77 cell | Growth inhibition assay | Inhibition of human ARH-77 cell growth in a cell viability assay.IC50=3.46915 μM | ||||
| SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay.IC50=4.49954 μM | ||||
| BB65-RCC cell | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay.IC50=0.08227 μM | ||||
| BB49-HNC cell | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay.IC50=0.38599 μM | ||||
| BC-1 cell | Growth inhibition assay | Inhibition of human BC-1 cell growth in a cell viability assay.IC50=28.651 μM | ||||
| BC-3 cell | Growth inhibition assay | Inhibition of human BC-3 cell growth in a cell viability assay.IC50=12.1138 μM | ||||
| BL-41 cell | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay.IC50=0.29123 μM | ||||
| BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay.IC50=0.0000008218 μM | ||||
| SW684 cell | Growth inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay.IC50=0.3498 μM | ||||
| BOKU cell | Growth inhibition assay | Inhibition of human BOKU cell growth in a cell viability assay.IC50=0.49133 μM | ||||
| SW954 cell | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay.IC50=0.02927 μM | ||||
| C2BBe1 cell | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay.IC50=0.08308 μM | ||||
| BV-173 cell | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay.IC50=0.000000109 μM | ||||
| Becker cell | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay.IC50=0.03003 μM | ||||
| SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay.IC50=0.01115 μM | ||||
| 697 cell | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay.IC50=0.19987 μM | ||||
| TE-15 cell | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay.IC50=0.005891 μM | ||||
| TE-11 cell | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay.IC50=0.07858 μM | ||||
| TE-5 cell | Growth inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay.IC50=1.79139 μM | ||||
| TE-6 cell | Growth inhibition assay | Inhibition of human TE-6 cell growth in a cell viability assay.IC50=1.21226 μM | ||||
| TE-9 cell | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay.IC50=0.87532 μM | ||||
| TGBC24TKB cell | Growth inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay.IC50=0.04761 μM | ||||
| TGW cell | Growth inhibition assay | Inhibition of human TGW cell growth in a cell viability assay.IC50=11.2828 μM | ||||
| TK10 cell | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay.IC50=0.01174 μM | ||||
| TGBC1TKB cell | Growth inhibition assay | Inhibition of human TGBC1TKB cell growth in a cell viability assay.IC50=0.06164 μM | ||||
| A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay.IC50=0.07284 μM | ||||
| UACC-257 cell | Growth inhibition assay | Inhibition of human UACC-257 cell growth in a cell viability assay.IC50=12.9198 μM | ||||
| U-87-MG cell | Growth inhibition assay | Inhibition of human U-87-MG cell growth in a cell viability assay.IC50=30.766 μM | ||||
| BB30-HNC cell | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay.IC50=0.05437 μM | ||||
| no-10 cell | Growth inhibition assay | Inhibition of human no-10 cell growth in a cell viability assay.IC50=0.31931 μM | ||||
| CAS-1 cell | Growth inhibition assay | Inhibition of human CAS-1 cell growth in a cell viability assay.IC50=1.40992 μM | ||||
| CGTH-W-1 cell | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay.IC50=0.03548 μM | ||||
| TE-10 cell | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay.IC50=0.06357 μM | ||||
| COLO-684 cell | Growth inhibition assay | Inhibition of human COLO-684 cell growth in a cell viability assay.IC50=46.2258 μM | ||||
| TE-12 cell | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay.IC50=0.01861 μM | ||||
| COR-L279 cell | Growth inhibition assay | Inhibition of human COR-L279 cell growth in a cell viability assay.IC50=40.2852 μM | ||||
| TE-8 cell | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay.IC50=0.01576 μM | ||||
| CP66-MEL cell | Growth inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay.IC50=0.19531 μM | ||||
| CTV-1 cell | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay.IC50=0.00004036 μM | ||||
| VA-ES-BJ cell | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay.IC50=0.03902 μM | ||||
| D-263MG cell | Growth inhibition assay | Inhibition of human D-263MG cell growth in a cell viability assay.IC50=0.36224 μM | ||||
| D-336MG cell | Growth inhibition assay | Inhibition of human D-336MG cell growth in a cell viability assay.IC50=0.006298 μM | ||||
| D-502MG cell | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay.IC50=1.23376 μM | ||||
| DJM-1 cell | Growth inhibition assay | Inhibition of human DJM-1 cell growth in a cell viability assay.IC50=6.48558 μM | ||||
| no-11 cell | Growth inhibition assay | Inhibition of human no-11 cell growth in a cell viability assay.IC50=0.50228 μM | ||||
| DMS-153 cell | Growth inhibition assay | Inhibition of human DMS-153 cell growth in a cell viability assay.IC50=14.0028 μM | ||||
| DSH1 cell | Growth inhibition assay | Inhibition of human DSH1 cell growth in a cell viability assay.IC50=0.24001 μM | ||||
| DU-4475 cell | Growth inhibition assay | Inhibition of human DU-4475 cell growth in a cell viability assay.IC50=8.21652 μM | ||||
| EB-3 cell | Growth inhibition assay | Inhibition of human EB-3 cell growth in a cell viability assay.IC50=34.3118 μM | ||||
| EHEB cell | Growth inhibition assay | Inhibition of human EHEB cell growth in a cell viability assay.IC50=10.0656 μM | ||||
| COLO-829 cell | Growth inhibition assay | Inhibition of human COLO-829 cell growth in a cell viability assay.IC50=0.12213 μM | ||||
| CP67-MEL cell | Growth inhibition assay | Inhibition of human CP67-MEL cell growth in a cell viability assay.IC50=0.20488 μM | ||||
| ES8 cell | Growth inhibition assay | Inhibition of human ES8 cell growth in a cell viability assay.IC50=32.1252 μM | ||||
| EVSA-T cell | Growth inhibition assay | Inhibition of human EVSA-T cell growth in a cell viability assay.IC50=9.27793 μM | ||||
| ES4 cell | Growth inhibition assay | Inhibition of human ES4 cell growth in a cell viability assay.IC50=1.05145 μM | ||||
| ETK-1 cell | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay.IC50=0.02832 μM | ||||
| ES6 cell | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay.IC50=0.03193 μM | ||||
| EW-24 cell | Growth inhibition assay | Inhibition of human EW-24 cell growth in a cell viability assay.IC50=0.78165 μM | ||||
| EoL-1-cell cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay.IC50=0.00001309 μM | ||||
| Calu-6 cell | Growth inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay.IC50=3.05741 μM | ||||
| GAK cell | Growth inhibition assay | Inhibition of human GAK cell growth in a cell viability assay.IC50=31.2686 μM | ||||
| D-247MG cell | Growth inhibition assay | Inhibition of human D-247MG cell growth in a cell viability assay.IC50=6.12519 μM | ||||
| GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay.IC50=0.02157 μM | ||||
| GI-ME-N cell | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay.IC50=0.06118 μM | ||||
| GCIY cell | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay.IC50=0.09656 μM | ||||
| GT3TKB cell | Growth inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay.IC50=9.35546 μM | ||||
| HC-1 cell | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay.IC50=24.5551 μM | ||||
| HAL-01 cell | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay.IC50=19.7543 μM | ||||
| HCC1187 cell | Growth inhibition assay | Inhibition of human HCC1187 cell growth in a cell viability assay.IC50=35.8052 μM | ||||
| DEL cell | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay.IC50=41.9086 μM | ||||
| HCC1599 cell | Growth inhibition assay | Inhibition of human HCC1599 cell growth in a cell viability assay.IC50=32.3325 μM | ||||
| DOHH-2 cell | Growth inhibition assay | Inhibition of human DOHH-2 cell growth in a cell viability assay.IC50=0.01719 μM | ||||
| HCC2157 cell | Growth inhibition assay | Inhibition of human HCC2157 cell growth in a cell viability assay.IC50=37.9946 μM | ||||
| HCE-4 cell | Growth inhibition assay | Inhibition of human HCE-4 cell growth in a cell viability assay.IC50=0.26439 μM | ||||
| HCE-T cell | Growth inhibition assay | Inhibition of human HCE-T cell growth in a cell viability assay.IC50=1.56714 μM | ||||
| HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay.IC50=10.4776 μM | ||||
| EM-2 cell | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay.IC50=0.000001078 μM | ||||
| HT-144 cell | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay.IC50=0.53609 μM | ||||
| EW-16 cell | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay.IC50=0.76178 μM | ||||
| IA-LM cell | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay.IC50=12.4445 μM | ||||
| IST-MEL1 cell | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay.IC50=0.1345 μM | ||||
| IST-MES1 cell | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay.IC50=0.08552 μM | ||||
| GI-1 cell | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay.IC50=1.3622 μM | ||||
| IST-SL2 cell | Growth inhibition assay | Inhibition of human IST-SL2 cell growth in a cell viability assay.IC50=0.50302 μM | ||||
| JVM-2 cell | Growth inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay.IC50=2.36284 μM | ||||
| JVM-3 cell | Growth inhibition assay | Inhibition of human JVM-3 cell growth in a cell viability assay.IC50=37.2338 μM | ||||
| KALS-1 cell | Growth inhibition assay | Inhibition of human KALS-1 cell growth in a cell viability assay.IC50=0.0949 μM | ||||
| KARPAS-422 cell | Growth inhibition assay | Inhibition of human KARPAS-422 cell growth in a cell viability assay.IC50=0.33997 μM | ||||
| JiyoyeP-2003 cell | Growth inhibition assay | Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay.IC50=1.73466 μM | ||||
| KARPAS-45 cell | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay.IC50=7.51671 μM | ||||
| KGN cell | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay.IC50=0.01942 μM | ||||
| KLE cell | Growth inhibition assay | Inhibition of human KLE cell growth in a cell viability assay.IC50=0.11317 μM | ||||
| KNS-42 cell | Growth inhibition assay | Inhibition of human KNS-42 cell growth in a cell viability assay.IC50=1.24412 μM | ||||
| KNS-81-FD cell | Growth inhibition assay | Inhibition of human KNS-81-FD cell growth in a cell viability assay.IC50=23.146 μM | ||||
| KP-N-YS cell | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay.IC50=12.9283 μM | ||||
| HOP-62 cell | Growth inhibition assay | Inhibition of human HOP-62 cell growth in a cell viability assay.IC50=0.01834 μM | ||||
| KURAMOCHI cell | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay.IC50=0.03487 μM | ||||
| HUTU-80 cell | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay.IC50=0.3142 μM | ||||
| LAMA-84 cell | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay.IC50=0.000003207 μM | ||||
| LB1047-RCC cell | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay.IC50=0.009887 μM | ||||
| LB2518-MEL cell | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay.IC50=0.14162 μM | ||||
| LB373-MEL-D cell | Growth inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay.IC50=0.82508 μM | ||||
| LB771-HNC cell | Growth inhibition assay | Inhibition of human LB771-HNC cell growth in a cell viability assay.IC50=2.57551 μM | ||||
| LB996-RCC cell | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay.IC50=0.009912 μM | ||||
| LC-2-ad cell | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay.IC50=0.02586 μM | ||||
| J-RT3-T3-5 cell | Growth inhibition assay | Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay.IC50=8.96529 μM | ||||
| LP-1 cell | Growth inhibition assay | Inhibition of human LP-1 cell growth in a cell viability assay.IC50=7.54782 μM | ||||
| K-562 cell | Growth inhibition assay | Inhibition of human K-562 cell growth in a cell viability assay.IC50=0.0000002656 μM | ||||
| LS-123 cell | Growth inhibition assay | Inhibition of human LS-123 cell growth in a cell viability assay.IC50=0.14064 μM | ||||
| K5 cell | Growth inhibition assay | Inhibition of human K5 cell growth in a cell viability assay.IC50=0.16489 μM | ||||
| LS-411N cell | Growth inhibition assay | Inhibition of human LS-411N cell growth in a cell viability assay.IC50=48.4748 μM | ||||
| KG-1 cell | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay.IC50=4.60845 μM | ||||
| KINGS-1 cell | Growth inhibition assay | Inhibition of human KINGS-1 cell growth in a cell viability assay.IC50=0.16666 μM | ||||
| LXF-289 cell | Growth inhibition assay | Inhibition of human LXF-289 cell growth in a cell viability assay.IC50=0.03956 μM | ||||
| MC116 cell | Growth inhibition assay | Inhibition of human MC116 cell growth in a cell viability assay.IC50=0.1141 μM | ||||
| KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay.IC50=0.0273 μM | ||||
| KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay.IC50=0.11883 μM | ||||
| MEG-01 cell | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay.IC50=0.000009805 μM | ||||
| MFH-ino cell | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay.IC50=0.04724 μM | ||||
| L-540 cell | Growth inhibition assay | Inhibition of human L-540 cell growth in a cell viability assay.IC50=15.0671 μM | ||||
| MHH-NB-11 cell | Growth inhibition assay | Inhibition of human MHH-NB-11 cell growth in a cell viability assay.IC50=43.0818 μM | ||||
| MMAC-SF cell | Growth inhibition assay | Inhibition of human MMAC-SF cell growth in a cell viability assay.IC50=8.79307 μM | ||||
| LB2241-RCC cell | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay.IC50=9.02012 μM | ||||
| LB831-BLC cell | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay.IC50=0.04609 μM | ||||
| MOLT-16 cell | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay.IC50=29.6292 μM | ||||
| LC-1F cell | Growth inhibition assay | Inhibition of human LC-1F cell growth in a cell viability assay.IC50=27.3245 μM | ||||
| MOLT-4 cell | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay.IC50=26.6753 μM | ||||
| MZ1-PC cell | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay.IC50=0.03119 μM | ||||
| MONO-MAC-6 cell | Growth inhibition assay | Inhibition of human MONO-MAC-6 cell growth in a cell viability assay.IC50=8.27066 μM | ||||
| MZ2-MEL cell | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay.IC50=0.28537 μM | ||||
| MPP-89 cell | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay.IC50=0.04049 μM | ||||
| MZ7-mel cell | Growth inhibition assay | Inhibition of human MZ7-mel cell growth in a cell viability assay.IC50=0.47911 μM | ||||
| LOXIMVI cell | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay.IC50=0.31503 μM | ||||
| NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay.IC50=0.19295 μM | ||||
| NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay.IC50=19.4877 μM | ||||
| NB5 cell | Growth inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay.IC50=1.39827 μM | ||||
| NB17 cell | Growth inhibition assay | Inhibition of human NB17 cell growth in a cell viability assay.IC50=3.63847 μM | ||||
| NCCIT cell | Growth inhibition assay | Inhibition of human NCCIT cell growth in a cell viability assay.IC50=2.86616 μM | ||||
| NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay.IC50=0.14436 μM | ||||
| NCI-H1304 cell | Growth inhibition assay | Inhibition of human NCI-H1304 cell growth in a cell viability assay.IC50=28.1628 μM | ||||
| NCI-H1395 cell | Growth inhibition assay | Inhibition of human NCI-H1395 cell growth in a cell viability assay.IC50=42.0163 μM | ||||
| MHH-PREB-1 cell | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay.IC50=0.74469 μM | ||||
| MLMA cell | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay.IC50=0.14032 μM | ||||
| MN-60 cell | Growth inhibition assay | Inhibition of human MN-60 cell growth in a cell viability assay.IC50=15.1979 μM | ||||
| MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay.IC50=4.36454 μM | ||||
| NB6 cell | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay.IC50=9.92259 μM | ||||
| NCI-H1355 cell | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay.IC50=0.11028 μM | ||||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
Chemische Informationen, Lagerung & Stabilität
| Molekulargewicht | 506.02 | Formel | C22H28ClN7O3S |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 863127-77-9 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | BMS-354825 Monohydrate | Smiles | CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.O | ||
Löslichkeit
|
In vitro |
DMSO
: 100 mg/mL
(197.62 mM)
Water : Insoluble Ethanol : Insoluble |
Molaritätsrechner
Verdünnungsrechner
Molekulargewichtsrechner
|
In vivo |
|||||
In-vivo-Formulierungsrechner (Klare Lösung)
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
mg/kg
g
μL
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
Wirkmechanismus
| Targets/IC50/Ki |
Abl
(Cell-free assay) 0.6 nM
Src
(Cell-free assay) 0.8 nM
c-Kit (D816V)
(Cell-free assay) 37 nM
c-Kit (wt)
(Cell-free assay) 79 nM
|
|---|---|
| In vitro |
Dasatinib ist wirksamer als Imatinib bei der Hemmung der Proliferation von Ba/F3-Zellen, die Wildtyp-Bcr-Abl und Bcr-Abl-Mutanten exprimieren, mit Ausnahme von T315I. Dasatinib weist eine um zwei Log-Stufen (~325-fach) erhöhte Potenz im Vergleich zu Imatinib auf. Dasatinib hemmt potent die Wildtyp-Abl-Kinase und alle Mutanten außer T315I über einen engen Bereich. Dasatinib zielt direkt auf Wildtyp- und mutierte Abl-Kinase-Domänen ab und hemmt die Autophosphorylierung und Substratphosphorylierung in einer konzentrationsabhängigen Weise. Dasatinib zeigt eine 325-fach höhere Potenz im Vergleich zu Imatinib gegenüber Zellen, die Wildtyp-Bcr-Abl exprimieren. Der Prozentsatz der Kolonien von TgE-Knochenmarkzellen nimmt von 100 % in unbehandelten Vertiefungen auf 4,12 % in Dasatinib-behandelten Vertiefungen ab. In Anwesenheit von Dasatinib ist der Unterschied im Prozentsatz der Kolonien, die von WT- und TgE-Knochenmarkzellen gebildet werden, statistisch signifikant. Die Expression von LMP2A ist in der Lage, das Überleben und die Proliferation von B-Lymphozyten zu fördern, was durch die Hemmung von Lyn- und/oder c-Abl-Kinasen mittels Dasatinib gehemmt werden kann. Eine Dasatinib-Behandlung hemmt die Src-Signalübertragung, verringert das Wachstum und induziert einen Zellzyklusarrest und Apoptose in einer Untergruppe von Schilddrüsenkrebszellen. Die Behandlung mit steigenden Dosen von Dasatinib (0,019 μM bis 1,25 μM) über 3 Tage hemmt das Wachstum der Zelllinien C643, TPC1, BCPAP und SW1736 um etwa 50 % bei niedrigen nanomolaren Konzentrationen, während höhere Konzentrationen erforderlich sind, um das Wachstum der K1-Zelllinie zu hemmen. Die Behandlung mit 10 nM oder 50 nM Dasatinib führt zu einer 9-22%igen Zunahme der Zellen in der G1-Population unter BCPAP- und SW1736- sowie K1-Zellen und einer entsprechenden 7-18%igen Abnahme des Prozentsatzes der Zellen in der S-Phase.
|
| Kinase-Assay |
Kinase-Autophosphorylierungsassays
|
|
Kinase-Assays mit Wildtyp- und mutierten Glutathion-S-Transferase (GST)-Abl-Fusionsproteinen (c-Abl-Aminosäuren 220-498) werden durchgeführt. GST-Abl-Fusionsproteine werden vor Gebrauch von Glutathion-Sepharose-Kügelchen freigesetzt; die ATP-Konzentration beträgt 5 μM. Unmittelbar vor der Verwendung in Kinase-Autophosphorylierungs- und In-vitro-Peptidsubstratphosphorylierungsassays werden GST-Abl-Kinase-Domänen-Fusionsproteine mit LAR-Tyrosinphosphatase behandelt. Nach einer 1-stündigen Inkubation bei 30 °C wird die LAR-Phosphatase durch Zugabe von Natriumvanadat (1 mM) inaktiviert. Eine Immunoblot-Analyse, die unbehandelte GST-Abl-Kinase mit dephosphorylierter GST-Abl-Kinase vergleicht, wird routinemäßig mit dem Phosphotyrosin-spezifischen Antikörper 4G10 durchgeführt, um eine vollständige (>95%) Dephosphorylierung der Tyrosinreste zu bestätigen, und mit dem c-Abl-Antikörper CST 2862, um eine gleiche Beladung der GST-Abl-Kinase zu bestätigen. Der Dasatinib-Konzentrationsbereich wird für die Mutante T315I auf 1.000 nM erweitert. Dieselben Inhibitor-Konzentrationen werden für die In-vitro-Peptidsubstratphosphorylierungsassays verwendet. Die drei Inhibitoren werden über dieselben Konzentrationsbereiche gegen GST-Src-Kinase und GST-Lyn-Kinase getestet.
|
|
| In vivo |
Dasatinib kehrt die Splenomegalie bei LMP2A/MYC doppeltransgenen Mäusen um. Dasatinib verhindert spezifisch die Koloniebildung durch LMP2A-exprimierende Knochenmark-B-Zellen und verringerte die Milzgröße bei den TgE-Mäusen. Die Milzmasse war bei Dasatinib-behandelten Tg6/λ-MYC-Mäusen im Vergleich zur Kontrollgruppe signifikant verringert. Dasatinib hemmt die Lymphadenopathie bei LMP2A/MYC doppeltransgenen Mäusen. Dasatinib kehrt die Splenomegalie bei Rag1KO-Mäusen um, die mit Tumorzellen von LMP2A/MYC doppeltransgenen Mäusen transplantiert wurden. Die Dasatinib-Therapie hemmt die Lyn-Phosphorylierung in B-Lymphozyten-Tumoren, die LMP2A exprimieren.
|
Literatur |
|
Anwendungen
| Methoden | Biomarker | Bilder | PMID |
|---|---|---|---|
| Western blot | phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 cleaved caspase 3 p-FAK/p-STAT3 |
|
23049975 |
| Growth inhibition assay | Cell viability |
|
23721490 |
| Immunofluorescence | SRC / Met α-tubulin F-actin / Actinin-4 / Paxillin |
|
26517812 |
| ELISA | TNF-α E-selectin VCAM-1 |
|
17684099 |
Klinische Studieninformationen
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT05527418 | Recruiting | Recent HIV-1 Infection |
Eva Bonfill|Institut d''Investigacions Biomèdiques August Pi i Sunyer |
January 26 2024 | Phase 2 |
| NCT05993949 | Recruiting | Lymphoblastic Leukemia |
Stanford University|Kite Pharma |
October 2 2023 | Phase 1 |
| NCT05780073 | Recruiting | HIV Infection Primary |
Fundació Institut Germans Trias i Pujol|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia|Spanish Clinical Research Network - SCReN|IrsiCaixa|University of Turin Italy|Instituto de Salud Carlos III|Germans Trias i Pujol Hospital |
October 16 2023 | Phase 2 |
| NCT05198843 | Terminated | Anatomic Stage IV Breast Cancer AJCC v8|Metastatic Triple-Negative Breast Inflammatory Carcinoma |
National Cancer Institute (NCI) |
November 8 2022 | Phase 1|Phase 2 |
| NCT04925648 | Recruiting | Metastatic Prostate Cancer |
St Vincent''s Hospital Sydney |
October 18 2021 | Phase 2 |
Technischer Support
Tel: +1-832-582-8158 Ext:3
Wenn Sie weitere Fragen haben, hinterlassen Sie bitte eine Nachricht.
Häufig gestellte Fragen
Frage 1:
What's the difference between S1021 and S7782?
Antwort:
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than it (S7782).
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