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PD-0332991 (Palbociclib) Hydrochloride CDK4/6 Inhibitor
Kat.-Nr.S1116
Chemische Struktur
Molekulargewicht: 483.99
Springe zu
Qualitätskontrolle (Quality Control)
Charge:
Reinheit:
99.99%
99.99
Produkte, die oft zusammen verwendet werden mit PD-0332991 (Palbociclib) Hydrochloride
Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| MOLM13 | Kinase Assay | 24 h | Inhibition of CDK4 assessed as inhibition of Rb phosphorylation with IC50 of 0.002 μM | 24641103 | ||
| COLO205 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.036 μM | 24641103 | ||
| U937 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.14 μM | 24641103 | ||
| MOLM13 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM | 24641103 | ||
| MOLM13 | Growth Inhibition Assay | 72 h | Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM | 24641103 | ||
| MDA-MB-435 | Growth Inhibition Assay | 24 h | IC50=0.16 μM | 15801831 | ||
| K562 | Cytotoxic Assay | 96 h | DMSO | IC50=2 μM | 24417566 | |
| DU145 | Cytotoxic Assay | 96 h | DMSO | IC50=7.5 μM | 24417566 | |
| MDA-MB-231 | Growth Inhibition Assay | 1 μM | 24 h | DMSO | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MCF7 | Growth Inhibition Assay | 1 μM | 24 h | DMSO | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MCF7 | Kinase Assay | 5 μM | 24 h | DMSO | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MDA-MB-231 | Kinase Assay | 5 μM | 24 h | DMSO | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MDA-MB-231 | Function Assay | 1-10 μM | 24 h | DMSO | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MCF7 | Function Assay | 1-10 μM | 24 h | DMSO | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MDA-MB-231 | Function Assay | 0.5-1 μM | 48 h | DMSO | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MCF7 | Function Assay | 0.5-1 μM | 48 h | DMSO | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MOLM13 | CDK4 inhibition assay | 24 h | IC50 = 0.011 μM | 24641103 | ||
| A2780 | Growth inhibition assay | 72 h | GI50 = 0.032 μM | 28156111 | ||
| COLO205 | Antiproliferative activity assay | 72 h | IC50 = 0.036 μM | 24641103 | ||
| MV4-11 | Growth inhibition assay | 72 h | GI50 = 0.05 μM | 28156111 | ||
| MOLM13 | Growth inhibition assay | 72 h | GI50 = 0.062 μM | 28156111 | ||
| NB4 | Growth inhibition assay | 72 h | GI50 = 0.066 μM | 28156111 | ||
| PC3 | Growth inhibition assay | 72 h | GI50 = 0.071 μM | 28156111 | ||
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | ||
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | ||
| MDA-MB-453 | Cytotoxicity assay | 48 h | IC50 = 0.137 μM | 27448913 | ||
| U937 | Antiproliferative activity assay | 72 h | IC50 = 0.14 μM | 24641103 | ||
| MDA-MB-435 | Antiproliferative activity assay | 24 h | IC50 = 0.16 μM | 26115571 | ||
| MCF7 | Cytotoxicity assay | 48 h | IC50 = 0.24 μM | 27448913 | ||
| MDA-MB-453 | Growth inhibition assay | 72 h | GI50 = 0.326 μM | 28156111 | ||
| MCF7 | Growth inhibition assay | 72 h | GI50 = 0.557 μM | 28156111 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 h | IC50 = 0.58 μM | 27448913 | ||
| M229 | Growth inhibition assay | 72 h | GI50 = 1.22 μM | 28156111 | ||
| M238 | Growth inhibition assay | 72 h | GI50 = 1.97 μM | 28156111 | ||
| M249 | Growth inhibition assay | 72 h | GI50 = 1.99 μM | 28156111 | ||
| K562 | Cytotoxicity assay | 96 h | IC50 = 2 μM | 24417566 | ||
| M249R | Growth inhibition assay | 72 h | GI50 = 2.96 μM | 28156111 | ||
| MOLM13 | FLT3 inhibition assay | 24 h | IC50 = 3 μM | 24641103 | ||
| MDA-MB-468 | Antiproliferative activity assay | 24 h | IC50 = 3 μM | 26115571 | ||
| C4-2B | Growth inhibition assay | 72 h | GI50 = 4.15 μM | 28156111 | ||
| DU145 | Growth inhibition assay | 72 h | GI50 = 5.792 μM | 28156111 | ||
| MDA-MB-468 | Growth inhibition assay | 72 h | GI50 = 5.96 μM | 28156111 | ||
| BPH1 | Growth inhibition assay | 72 h | GI50 = 7.442 μM | 28156111 | ||
| DU145 | Cytotoxicity assay | 96 h | IC50 = 7.5 μM | 24417566 | ||
| MRC5 | Growth inhibition assay | 72 h | GI50 = 10 μM | 28156111 | ||
| 697 | Growth Inhibition Assay | IC50=148.38 nM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=96.04 nM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=161.8 nM | SANGER | |||
| EoL-1 | Growth Inhibition Assay | IC50=187.26 nM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=198.25 nM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=220.02 nM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=220.19 nM | SANGER | |||
| AsPC-1 | Growth Inhibition Assay | IC50=252.53 nM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=256.25 nM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=258.19 nM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=258.49 nM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=273.09 nM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=314.1 nM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=321.05 nM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=340.66 nM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=345.13 nM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=376.16 nM | SANGER | |||
| SK-N-AS | Growth Inhibition Assay | IC50=387.83 nM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=405.02 nM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=411.89 nM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=432.95 nM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=444.27 nM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=466.9 nM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=483.58 nM | SANGER | |||
| CAL-27 | Growth Inhibition Assay | IC50=494.59 nM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=495.43 nM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=504.73 nM | SANGER | |||
| PA-1 | Growth Inhibition Assay | IC50=509.86 nM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=513.85 nM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=521.62 nM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=526.86 nM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=564.99 nM | SANGER | |||
| CHP-212 | Growth Inhibition Assay | IC50=593.59 nM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=599.18 nM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=599.43 nM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=603.52 nM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=605.21 nM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=605.67 nM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=633.91 nM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=636.99 nM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=650.64 nM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=652.48 nM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=677.82 nM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=695.54 nM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=717.12 nM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=728.93 nM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=732.27 nM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=742.99 nM | SANGER | |||
| NCI-H520 | Growth Inhibition Assay | IC50=746.52 nM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=752.8 nM | SANGER | |||
| T-24 | Growth Inhibition Assay | IC50=778.71 nM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=808.63 nM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=808.76 nM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=812.79 nM | SANGER | |||
| U251 | Growth Inhibition Assay | IC50=813.88 nM | SANGER | |||
| CAMA-1 | Growth Inhibition Assay | IC50=833.94 nM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=851.78 nM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=897.78 nM | SANGER | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=900.1 nM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=927.56 nM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=929.41 nM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=936.06 nM | SANGER | |||
| Mewo | Growth Inhibition Assay | IC50=936.6 nM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=940.55 nM | SANGER | |||
| HO-1-N-1 | Growth Inhibition Assay | IC50=962.81 nM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=966.48 nM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=998.25 nM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=1.00076 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=1.00875 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=1.01421 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=1.04812 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=1.07273 μM | SANGER | |||
| CAL-39 | Growth Inhibition Assay | IC50=1.07522 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=1.08408 μM | SANGER | |||
| CHP-134 | Growth Inhibition Assay | IC50=1.11807 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=1.12395 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.13134 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=1.16354 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=1.17186 μM | SANGER | |||
| MHH-ES-1 | Growth Inhibition Assay | IC50=1.17986 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.1862 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=1.20734 μM | SANGER | |||
| COR-L23 | Growth Inhibition Assay | IC50=1.22933 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=1.24267 μM | SANGER | |||
| Hs-578-T | Growth Inhibition Assay | IC50=1.25817 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=1.26686 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=1.29338 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=1.29399 μM | SANGER | |||
| COLO-741 | Growth Inhibition Assay | IC50=1.32089 μM | SANGER | |||
| PC-3 | Growth Inhibition Assay | IC50=1.35221 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=1.35296 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=1.37519 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=1.41774 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=1.46923 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=1.50528 μM | SANGER | |||
| HN | Growth Inhibition Assay | IC50=1.54071 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=1.54907 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.58507 μM | SANGER | |||
| CAL-62 | Growth Inhibition Assay | IC50=1.60862 μM | SANGER | |||
| MG-63 | Growth Inhibition Assay | IC50=1.61813 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=1.62152 μM | SANGER | |||
| BCPAP | Growth Inhibition Assay | IC50=1.66457 μM | SANGER | |||
| 22RV1 | Growth Inhibition Assay | IC50=1.67843 μM | SANGER | |||
| T47D | Growth Inhibition Assay | IC50=1.68061 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=1.69603 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=1.70273 μM | SANGER | |||
| H4 | Growth Inhibition Assay | IC50=1.73212 μM | SANGER | |||
| CAL-51 | Growth Inhibition Assay | IC50=1.74855 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=1.78582 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=1.79542 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=1.81061 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=1.81602 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=1.87412 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=1.89282 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=1.91228 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=1.92428 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=1.96246 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=1.9833 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=1.99323 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=2.00666 μM | SANGER | |||
| SW1710 | Growth Inhibition Assay | IC50=2.06945 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition Assay | IC50=2.07298 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=2.08951 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=2.15439 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=2.20374 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=2.20413 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=2.23122 μM | SANGER | |||
| SW620 | Growth Inhibition Assay | IC50=2.26169 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=2.3106 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=2.32058 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=2.32199 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=2.35374 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=2.36437 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=2.37796 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=2.38496 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=2.40374 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=2.45422 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=2.46883 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=2.52773 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=2.55951 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=2.59199 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition Assay | IC50=2.59266 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=2.59394 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition Assay | IC50=2.61803 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=2.62057 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=2.70206 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=2.71464 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=2.7243 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition Assay | IC50=2.75694 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=2.77099 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=2.81884 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=2.82505 μM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=2.85053 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=2.95832 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=3.05263 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=3.0543 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=3.20165 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=3.36488 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=3.44079 μM | SANGER | |||
| DU-145 | Growth Inhibition Assay | IC50=3.46269 μM | SANGER | |||
| SW1088 | Growth Inhibition Assay | IC50=3.4747 μM | SANGER | |||
| HOP-92 | Growth Inhibition Assay | IC50=3.50342 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=3.62139 μM | SANGER | |||
| NCI-H460 | Growth Inhibition Assay | IC50=3.6673 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=3.72535 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=3.76936 μM | SANGER | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=3.81951 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=3.832 μM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=4.018 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=4.02302 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=4.02461 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=4.18556 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition Assay | IC50=4.31284 μM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=4.32169 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=4.33153 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=4.50092 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=4.52231 μM | SANGER | |||
| BEN | Growth Inhibition Assay | IC50=4.52815 μM | SANGER | |||
| BFTC-909 | Growth Inhibition Assay | IC50=4.56275 μM | SANGER | |||
| NCI-H2087 | Growth Inhibition Assay | IC50=4.58164 μM | SANGER | |||
| RVH-421 | Growth Inhibition Assay | IC50=4.6669 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=4.68008 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=4.81661 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=4.83016 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=4.85926 μM | SANGER | |||
| OE33 | Growth Inhibition Assay | IC50=4.88161 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=4.95061 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=5.02983 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=5.06194 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=5.09889 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=5.18709 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=5.19416 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=5.24622 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=5.25942 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=5.30634 μM | SANGER | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=5.31808 μM | SANGER | |||
| S-117 | Growth Inhibition Assay | IC50=5.36976 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=5.39681 μM | SANGER | |||
| NCI-H2122 | Growth Inhibition Assay | IC50=5.49397 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=5.67593 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=5.70088 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=5.80556 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=5.917 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=5.91932 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=5.9836 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=6.00422 μM | SANGER | |||
| KU-19-19 | Growth Inhibition Assay | IC50=6.01731 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition Assay | IC50=6.04443 μM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=6.05063 μM | SANGER | |||
| 8505C | Growth Inhibition Assay | IC50=6.07573 μM | SANGER | |||
| GMS-10 | Growth Inhibition Assay | IC50=6.15002 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=6.1671 μM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=6.22072 μM | SANGER | |||
| FADU | Growth Inhibition Assay | IC50=6.26039 μM | SANGER | |||
| BxPC-3 | Growth Inhibition Assay | IC50=6.2732 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=6.29201 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=6.31512 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=6.33455 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=6.382 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=6.38447 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=6.42376 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=6.51023 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=6.56147 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=6.60076 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=6.62215 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=6.75044 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=6.76117 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=6.78197 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=6.938 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=7.0633 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=7.07881 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=7.18371 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=7.20601 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=7.22127 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=7.30309 μM | SANGER | |||
| EW-22 | Growth Inhibition Assay | IC50=7.34348 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=7.35162 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=7.4402 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=7.49899 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=7.52594 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=7.55515 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=7.5951 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=7.62279 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=7.62957 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=7.65368 μM | SANGER | |||
| KYSE-180 | Growth Inhibition Assay | IC50=7.71169 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=7.95971 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=7.98551 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=8.012 μM | SANGER | |||
| SW1990 | Growth Inhibition Assay | IC50=8.04659 μM | SANGER | |||
| EFM-19 | Growth Inhibition Assay | IC50=8.08545 μM | SANGER | |||
| OGR-1 | Growth Inhibition Assay | IC50=8.43023 μM | SANGER | |||
| U-118-MG | Growth Inhibition Assay | IC50=8.43463 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=8.46765 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=8.51761 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=8.57635 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=8.70484 μM | SANGER | |||
| RPMI-2650 | Growth Inhibition Assay | IC50=8.71955 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=8.74307 μM | SANGER | |||
| KYSE-450 | Growth Inhibition Assay | IC50=8.86548 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=9.14058 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=9.31979 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=9.35778 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=9.36701 μM | SANGER | |||
| AN3-CA | Growth Inhibition Assay | IC50=9.45444 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=9.72849 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=9.76629 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=9.79369 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=9.83664 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=9.98746 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=10.0396 μM | SANGER | |||
| NCI-H650 | Growth Inhibition Assay | IC50=10.4286 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=10.455 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=11.0515 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=11.1446 μM | SANGER | |||
| CO-314 | Growth Inhibition Assay | IC50=11.2842 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=11.5323 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=11.5527 μM | SANGER | |||
| SW1463 | Growth Inhibition Assay | IC50=11.5989 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=11.6552 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=11.7197 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=12.1495 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=12.2856 μM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=12.3801 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=12.717 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=12.9482 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=13.1284 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=13.2651 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=13.2893 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=13.3037 μM | SANGER | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=13.3728 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=13.4067 μM | SANGER | |||
| SNU-387 | Growth Inhibition Assay | IC50=13.5072 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=13.6718 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=13.707 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=13.7992 μM | SANGER | |||
| CAN | Growth Inhibition Assay | IC50=14.0288 μM | SANGER | |||
| SK-MEL-30 | Growth Inhibition Assay | IC50=14.063 μM | SANGER | |||
| COLO-678 | Growth Inhibition Assay | IC50=14.0822 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=14.1021 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=14.1402 μM | SANGER | |||
| SL-513 | Growth Inhibition Assay | IC50=14.187 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=14.3852 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=14.4435 μM | SANGER | |||
| KYSE-140 | Growth Inhibition Assay | IC50=14.6327 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=14.8001 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=15.0625 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=15.4662 μM | SANGER | |||
| COLO-679 | Growth Inhibition Assay | IC50=15.7683 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=16.1201 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=16.3523 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=16.7071 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition Assay | IC50=17.2448 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=17.3808 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=17.7503 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=17.7716 μM | SANGER | |||
| HuP-T4 | Growth Inhibition Assay | IC50=18.0206 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=18.1402 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=18.1697 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=18.2254 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=18.5094 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=18.6051 μM | SANGER | |||
| EPLC-272H | Growth Inhibition Assay | IC50=19.0434 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=19.045 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=19.2123 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=19.6804 μM | SANGER | |||
| KYSE-410 | Growth Inhibition Assay | IC50=19.9139 μM | SANGER | |||
| HuCCT1 | Growth Inhibition Assay | IC50=20.6294 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=20.7168 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=20.8059 μM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=20.915 μM | SANGER | |||
| Capan-2 | Growth Inhibition Assay | IC50=21.0413 μM | SANGER | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=21.2515 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=21.3081 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=21.3342 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=21.5716 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=21.6618 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=21.9825 μM | SANGER | |||
| AM-38 | Growth Inhibition Assay | IC50=22.0485 μM | SANGER | |||
| A431 | Growth Inhibition Assay | IC50=23.2119 μM | SANGER | |||
| YAPC | Growth Inhibition Assay | IC50=23.2651 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=23.4809 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=23.4937 μM | SANGER | |||
| SCC-25 | Growth Inhibition Assay | IC50=24.3006 μM | SANGER | |||
| HT-29 | Growth Inhibition Assay | IC50=24.3823 μM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=24.6571 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=25.5071 μM | SANGER | |||
| SJRH30 | Growth Inhibition Assay | IC50=25.6496 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=26.1629 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=26.3645 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=26.4491 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=26.6541 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=26.9397 μM | SANGER | |||
| HCC1954 | Growth Inhibition Assay | IC50=26.9808 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=27.4163 μM | SANGER | |||
| LU-99A | Growth Inhibition Assay | IC50=27.5582 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=27.7299 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition Assay | IC50=27.7775 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition Assay | IC50=27.9387 μM | SANGER | |||
| MDA-MB-415 | Growth Inhibition Assay | IC50=28.4137 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=28.5281 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=28.7117 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=28.9261 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=31.0494 μM | SANGER | |||
| Saos-2 | Growth Inhibition Assay | IC50=31.9306 μM | SANGER | |||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.8231 μM | SANGER | |||
| M14 | Growth Inhibition Assay | IC50=32.9764 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=33.5011 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=34.3305 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=35.8674 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=36.0427 μM | SANGER | |||
| CP50-MEL-B | Growth Inhibition Assay | IC50=36.1911 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=36.452 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=36.8099 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=37.1417 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=37.2484 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=38.0691 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=38.4714 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=39.242 μM | SANGER | |||
| OVACR-3 | Growth Inhibition Assay | IC50=39.9195 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=40.4258 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=41.2415 μM | SANGER | |||
| C3A | Growth Inhibition Assay | IC50=41.3447 μM | SANGER | |||
| HT55 | Growth Inhibition Assay | IC50=42.2841 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=42.2974 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=42.4616 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=43.9892 μM | SANGER | |||
| JEG-3 | Growth Inhibition Assay | IC50=44.947 μM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=46.3998 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=47.2898 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=47.4188 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=47.492 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=48.0715 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=49.4228 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=49.5119 μM | SANGER | |||
| NCI-H1651 | Growth Inhibition Assay | IC50=49.8821 μM | SANGER | |||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)
| Molekulargewicht | 483.99 | Formel | C24H29N7O2.HCl |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 827022-32-2 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | N/A | Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl | ||
Löslichkeit (Solubility)
|
In vitro |
Water : 50 mg/mL
DMSO
: 13 mg/mL
(26.86 mM)
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 (Mechanism of Action)
| Merkmale |
Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
|
|---|---|
| Targets/IC50/Ki |
CDK4/CyclinD3
(Cell-free assay) 9 nM
CDK4/CyclinD1
(Cell-free assay) 11 nM
CDK6/CyclinD2
(Cell-free assay) 15 nM
|
| In vitro |
PD 0332991 hat nur geringe Auswirkungen auf andere Proteinkinasen, einschließlich EGFR, FGFR, PGFR, IR. PD 0332991 ist ein nicht-ATP-kompetitiver Inhibitor von Cdk4. PD 0332991 hemmt MDA-MB-435-Brustkarzinomzellen mit einer IC50 von 66 nM, was auf eine reduzierte Rb-Phosphorylierung an Ser780 zurückzuführen ist. PD 0332991 hemmt den Einbau von Thymidin in die DNA von Rb-positiven menschlichen Brust-, Darm- und Lungenkarzinomen sowie menschlichen Leukämien mit IC50-Werten im Bereich von 0,04-0,17 μM. PD 0332991 zeigt keine Aktivität in Rb-negativen Zellen. PD 0332991 verursacht eine Akkumulation von Zellen in G1 in MDA-MB-453-Brust- und Colo-205-Karzinomzellen. PD 0332991 zeigt auch Aktivität in 5T33MM-Myelomzellen (immunkompetentes Modell) und sensibilisiert die Zellen für die Abtötung durch Bortezomib. PD 0332991 hemmt luminale ER-positive sowie HER2-amplifizierte Brustkrebszelllinien einschließlich MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 und UACC-893. PD 0332991 verstärkt die Aktivität von Tamoxifen und Trastuzumab in diesen Zelllinien. PD 0332991 erhöht die Empfindlichkeit von Tamoxifen in den MCF7-Tamoxifen-resistenten Zellen. Eine aktuelle Studie zeigt, dass PD 0332991 maligne rhabdoide Tumorzelllinien (MRT-Zellen) einschließlich MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS unterdrücken könnte und die Empfindlichkeit der MRT-Zelllinien gegenüber PD 0332991 umgekehrt mit der Expression von p16 korreliert.
|
| Kinase-Assay |
Cdk-Assays
|
|
Eine Stammlösung von PD0332991 wird in DMSO hergestellt. CDK-Assays werden in 96-Well-Filterplatten durchgeführt. Alle CDK-Cyclin-Kinase-Komplexe werden in Insektenzellen durch Baculovirus-Infektion exprimiert und gereinigt. Das Substrat für die Assays ist ein Fragment (Aminosäuren 792–928) von pRb, fusioniert an GST (GST·RB-Cterm). Das Gesamtvolumen in jedem Well beträgt 0,1 ml und enthält eine Endkonzentration von 20 mM Tris-HCl, pH 7,4, 50 mM NaCl, 1 mM Dithiothreitol, 10 mM MgCl2, 25 μM ATP (für CDK4-Cyclin D1, CDK6-Cyclin D2 und CDK6-Cyclin D3) oder 12 μM ATP (für CDK2-Cyclin E, CDK2-Cyclin A und CDC2-Cyclin B) mit 0,25 μCi [γ-32P]ATP, 20 ng Enzym, 1 μg GST·RB-Cterm und PD 0332991 (0,001-0,1 μM). Alle Komponenten außer dem [γ-32P]ATP werden zu den Wells gegeben, und die Platte wird 2 Minuten lang auf einem Plattenmischer platziert. Die Reaktion wird durch Zugabe des [γ-32P]ATP gestartet und die Platte wird 15 Minuten lang bei 25 °C inkubiert. Die Reaktion wird durch Zugabe von 0,1 ml 20%iger Trichloressigsäure beendet und die Platte wird mindestens 1 Stunde lang bei 4 °C aufbewahrt, damit das Substrat präzipitieren kann. Die Wells werden dann 5 Mal mit 0,2 ml 10%iger Trichloressigsäure gewaschen und der radioaktive Einbau wird mit einem β-Plattenzähler bestimmt.
|
|
| In vivo |
PD 0332991 zeigt eine vollständige Tumorstase in einem MDA-MB-435-Xenotransplantat bei 150 mg/kg. PD 0332991 zeigt auch eine breitbandige Antitumoraktivität in mehreren menschlichen Tumor-Xenotransplantaten, indem es Phospho-Rb und den Proliferationsmarker Ki-67 aus dem Tumorgewebe eliminiert und die Genexpression unter der transkriptionellen Kontrolle von E2F herunterreguliert.
|
Literatur |
|
Anwendungen (Applications)
| Methoden | Biomarker | Bilder | PMID |
|---|---|---|---|
| Western blot | RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO pRb(S807, 811) / CDK4 / CDK6 / PARP LC3-I / LC3-II pAMPKα(T172) / pULK1(S317) SMAD2 (pS255) |
|
30300583 |
| Growth inhibition assay | Cell viability |
|
29670090 |
| Immunofluorescence | SAHF/ATRX LC3B |
|
26988987 |
| ELISA | PGE2 |
|
26540629 |
Klinische Studieninformationen (Clinical Trial Information)
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT05665361 | Recruiting | Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc) |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
April 24 2024 | Phase 1|Phase 2 |
| NCT06307457 | Completed | Breast Cancer |
Pfizer |
March 11 2024 | -- |
| NCT05912933 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
| NCT05709158 | Not yet recruiting | Breast Cancer |
Pfizer |
March 1 2024 | -- |
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