Home Apoptosis Bcl-2 Inhibitor Navitoclax (ABT-263)

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Navitoclax (ABT-263) Bcl-2 Inhibitor

Kat.-Nr.S1001

Als potenter Inhibitor von Bcl-xL, Bcl-2 und Bcl-w mit Ki von ≤ 0,5 nM, ≤1 nM und ≤1 nM in zellfreien Assays, bindet Navitoclax (ABT-263) schwächer an Mcl-1 und A1. Phase 2.
Navitoclax (ABT-263) Bcl-2 Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 974.61

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Qualitätskontrolle

Charge: Reinheit: 99.86%
99.86

Produkte, die oft zusammen verwendet werden mit Navitoclax (ABT-263)

A-1331852

It and A-1331852 selectively induce apoptosis in senescent endothelial cells (ECs).

ABT-737

It and ABT-737 induce BAK/BAX-mediated platelet apoptosis by pharmacologically suppressing BCL-XL.

MG132

This compound and MG132 plus GX15-070 partially restore the protein expression of Bcl-2-associated athanogene domain 3 (Bag3) and the deubiquitinase Usp9X in LN229 glioblastoma cells.

Y-27632 Dihydrochloride

It and Y-27632 2HCl synergistically enhance mitochondrial priming and provide a potential therapeutic strategy for scleroderma fibroblast apoptosis.

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
FL5.12 Cytotoxicity assay 24 h EC50 = 0.0042 μM 18841882
FL5.12 Cytotoxicity assay 24 h EC50 = 0.0059 μM 18841882
RS4:11 Apoptosis assay 6 h EC50 = 0.014 μM 24881567
FDC-P1 BCL-2 inhibition assay 24 h IC50 = 0.015 μM 24881567
NCI-H1963 Cytotoxicity assay 4 days IC50 = 0.0266 μM 23448298
NCI-H187 Cytotoxicity assay 4 days IC50 = 0.0384 μM 23448298
NCI-H1417 Cytotoxicity assay 4 days IC50 = 0.0542 μM 23448298
FDC-P1 BCL-xL inhibition assay 24 h IC50 = 0.06 μM 24881567
NCI-H146 Cytotoxicity assay 48 h EC50 = 0.0867 μM 18841882
RS4:11 Antiproliferative activity assay EC50 = 0.112 μM 28926247
MOLT4 Antiproliferative activity assay EC50 = 0.303 μM 28926247
EoL-1-cell Growth Inhibition Assay IC50=0.00669 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.01586 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.01699 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.01983 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.02314 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.02587 μM SANGER
HL-60 Growth Inhibition Assay IC50=0.02908 μM SANGER
KY821 Growth Inhibition Assay IC50=0.02975 μM SANGER
ECC10 Growth Inhibition Assay IC50=0.03792 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.04011 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.04287 μM SANGER
KG-1 Growth Inhibition Assay IC50=0.04486 μM SANGER
TGW Growth Inhibition Assay IC50=0.04633 μM SANGER
ATN-1 Growth Inhibition Assay IC50=0.04733 μM SANGER
RH-18 Growth Inhibition Assay IC50=0.06048 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.06841 μM SANGER
NB17 Growth Inhibition Assay IC50=0.07124 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.07213 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=0.07778 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.07815 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.08053 μM SANGER
NB13 Growth Inhibition Assay IC50=0.08203 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.08704 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=0.10275 μM SANGER
NH-12 Growth Inhibition Assay IC50=0.10744 μM SANGER
697 Growth Inhibition Assay IC50=0.10839 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.1137 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=0.15169 μM SANGER
CHP-134 Growth Inhibition Assay IC50=0.16306 μM SANGER
D-283MED Growth Inhibition Assay IC50=0.17686 μM SANGER
LU-135 Growth Inhibition Assay IC50=0.18552 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.18671 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.19918 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.20498 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.21988 μM SANGER
NB12 Growth Inhibition Assay IC50=0.23115 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=0.23573 μM SANGER
BEN Growth Inhibition Assay IC50=0.23968 μM SANGER
HCC1569 Growth Inhibition Assay IC50=0.25106 μM SANGER
HuO9 Growth Inhibition Assay IC50=0.26715 μM SANGER
WM-115 Growth Inhibition Assay IC50=0.27738 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=0.33529 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=0.35343 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.36459 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.3654 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=0.41023 μM SANGER
A704 Growth Inhibition Assay IC50=0.4267 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=0.44017 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=0.45652 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=0.45778 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=0.46157 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.46613 μM SANGER
EW-22 Growth Inhibition Assay IC50=0.46671 μM SANGER
MS-1 Growth Inhibition Assay IC50=0.46933 μM SANGER
RMG-I Growth Inhibition Assay IC50=0.49464 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.50019 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=0.50953 μM SANGER
SW1417 Growth Inhibition Assay IC50=0.55438 μM SANGER
DB Growth Inhibition Assay IC50=0.5708 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.5832 μM SANGER
EW-13 Growth Inhibition Assay IC50=0.58341 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.59207 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.60808 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.65264 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.65427 μM SANGER
HAL-01 Growth Inhibition Assay IC50=0.72549 μM SANGER
RD Growth Inhibition Assay IC50=0.75899 μM SANGER
OAW-28 Growth Inhibition Assay IC50=0.7837 μM SANGER
HCC38 Growth Inhibition Assay IC50=0.8019 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.81121 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.81328 μM SANGER
DU-145 Growth Inhibition Assay IC50=0.89923 μM SANGER
HPAF-II Growth Inhibition Assay IC50=0.92628 μM SANGER
A427 Growth Inhibition Assay IC50=0.93022 μM SANGER
PA-1 Growth Inhibition Assay IC50=0.95642 μM SANGER
OAW-42 Growth Inhibition Assay IC50=0.96146 μM SANGER
L-428 Growth Inhibition Assay IC50=1.0125 μM SANGER
COLO-824 Growth Inhibition Assay IC50=1.01708 μM SANGER
P30-OHK Growth Inhibition Assay IC50=1.04688 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=1.0623 μM SANGER
HCC2998 Growth Inhibition Assay IC50=1.07135 μM SANGER
NB14 Growth Inhibition Assay IC50=1.13748 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=1.14152 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=1.16236 μM SANGER
CAL-120 Growth Inhibition Assay IC50=1.16429 μM SANGER
SBC-1 Growth Inhibition Assay IC50=1.19053 μM SANGER
C32 Growth Inhibition Assay IC50=1.19088 μM SANGER
HCC2157 Growth Inhibition Assay IC50=1.19494 μM SANGER
COLO-792 Growth Inhibition Assay IC50=1.20071 μM SANGER
ES7 Growth Inhibition Assay IC50=1.27951 μM SANGER
HEL Growth Inhibition Assay IC50=1.31029 μM SANGER
ES4 Growth Inhibition Assay IC50=1.34998 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=1.36555 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=1.3885 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=1.40269 μM SANGER
NB69 Growth Inhibition Assay IC50=1.46271 μM SANGER
D-247MG Growth Inhibition Assay IC50=1.51122 μM SANGER
SCC-4 Growth Inhibition Assay IC50=1.59887 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.67293 μM SANGER
A388 Growth Inhibition Assay IC50=1.68724 μM SANGER
Calu-3 Growth Inhibition Assay IC50=1.70697 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=1.71418 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=1.72201 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=1.73656 μM SANGER
DEL Growth Inhibition Assay IC50=1.74692 μM SANGER
SNU-423 Growth Inhibition Assay IC50=1.78157 μM SANGER
COR-L23 Growth Inhibition Assay IC50=1.79874 μM SANGER
OMC-1 Growth Inhibition Assay IC50=1.86016 μM SANGER
EW-11 Growth Inhibition Assay IC50=1.95657 μM SANGER
HSC-3 Growth Inhibition Assay IC50=1.96365 μM SANGER
MLMA Growth Inhibition Assay IC50=1.96677 μM SANGER
RCM-1 Growth Inhibition Assay IC50=2.00399 μM SANGER
MFE-280 Growth Inhibition Assay IC50=2.02848 μM SANGER
ES8 Growth Inhibition Assay IC50=2.25471 μM SANGER
TE-11 Growth Inhibition Assay IC50=2.29473 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=2.4878 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=2.51158 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=2.57681 μM SANGER
HOP-92 Growth Inhibition Assay IC50=2.58743 μM SANGER
IGR-1 Growth Inhibition Assay IC50=2.62035 μM SANGER
GOTO Growth Inhibition Assay IC50=2.65377 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=2.72215 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=2.79681 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=2.82782 μM SANGER
U-118-MG Growth Inhibition Assay IC50=2.96491 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=3.01417 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=3.04997 μM SANGER
MPP-89 Growth Inhibition Assay IC50=3.05666 μM SANGER
GCIY Growth Inhibition Assay IC50=3.20491 μM SANGER
SW626 Growth Inhibition Assay IC50=3.24543 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=3.31272 μM SANGER
NBsusSR Growth Inhibition Assay IC50=3.34938 μM SANGER
AN3-CA Growth Inhibition Assay IC50=3.44238 μM SANGER
EFM-19 Growth Inhibition Assay IC50=3.48339 μM SANGER
RVH-421 Growth Inhibition Assay IC50=3.56877 μM SANGER
5637 Growth Inhibition Assay IC50=3.61103 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=3.63472 μM SANGER
H9 Growth Inhibition Assay IC50=3.67144 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=3.67361 μM SANGER
TE-5 Growth Inhibition Assay IC50=3.70709 μM SANGER
NOS-1 Growth Inhibition Assay IC50=3.79834 μM SANGER
HH Growth Inhibition Assay IC50=3.83868 μM SANGER
769-P Growth Inhibition Assay IC50=3.8951 μM SANGER
CHP-212 Growth Inhibition Assay IC50=3.92549 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=3.95936 μM SANGER
Mo-T Growth Inhibition Assay IC50=4.04312 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=4.04399 μM SANGER
SW1990 Growth Inhibition Assay IC50=4.05908 μM SANGER
LK-2 Growth Inhibition Assay IC50=4.11293 μM SANGER
ES5 Growth Inhibition Assay IC50=4.13985 μM SANGER
JVM-3 Growth Inhibition Assay IC50=4.18222 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=4.22413 μM SANGER
Calu-6 Growth Inhibition Assay IC50=4.27881 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=4.29568 μM SANGER
SW954 Growth Inhibition Assay IC50=4.2966 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=4.31831 μM SANGER
ES3 Growth Inhibition Assay IC50=4.35441 μM SANGER
no-11 Growth Inhibition Assay IC50=4.35554 μM SANGER
LAN-6 Growth Inhibition Assay IC50=4.45189 μM SANGER
FTC-133 Growth Inhibition Assay IC50=4.5395 μM SANGER
8505C Growth Inhibition Assay IC50=4.5423 μM SANGER
SW620 Growth Inhibition Assay IC50=4.57057 μM SANGER
BCPAP Growth Inhibition Assay IC50=4.63481 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=4.66089 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=4.70228 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=4.74008 μM SANGER
GP5d Growth Inhibition Assay IC50=4.78388 μM SANGER
NB6 Growth Inhibition Assay IC50=4.86204 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=4.8876 μM SANGER
UMC-11 Growth Inhibition Assay IC50=4.88964 μM SANGER
HCC1419 Growth Inhibition Assay IC50=4.90063 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=4.94185 μM SANGER
LXF-289 Growth Inhibition Assay IC50=5.03719 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=5.07744 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=5.23969 μM SANGER
ESS-1 Growth Inhibition Assay IC50=5.25597 μM SANGER
GI-1 Growth Inhibition Assay IC50=5.27926 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=5.3616 μM SANGER
IA-LM Growth Inhibition Assay IC50=5.39871 μM SANGER
KP-4 Growth Inhibition Assay IC50=5.46334 μM SANGER
G-402 Growth Inhibition Assay IC50=5.51865 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=5.52604 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=5.54955 μM SANGER
OE19 Growth Inhibition Assay IC50=5.68624 μM SANGER
U-2-OS Growth Inhibition Assay IC50=5.89013 μM SANGER
SCC-15 Growth Inhibition Assay IC50=5.93662 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=5.99404 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=6.05259 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=6.20874 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=6.42915 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=6.47625 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=6.62925 μM SANGER
SW780 Growth Inhibition Assay IC50=6.70185 μM SANGER
NEC8 Growth Inhibition Assay IC50=6.7663 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=6.78111 μM SANGER
COLO-668 Growth Inhibition Assay IC50=6.84387 μM SANGER
MC116 Growth Inhibition Assay IC50=6.93897 μM SANGER
HCC1937 Growth Inhibition Assay IC50=6.99251 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=7.19293 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=7.22738 μM SANGER
HCC1806 Growth Inhibition Assay IC50=7.26044 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=7.33038 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=7.39694 μM SANGER
SW1783 Growth Inhibition Assay IC50=7.43175 μM SANGER
GCT Growth Inhibition Assay IC50=7.56906 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=7.73625 μM SANGER
MEL-HO Growth Inhibition Assay IC50=7.77054 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=7.77357 μM SANGER
SW756 Growth Inhibition Assay IC50=7.78333 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=7.81892 μM SANGER
HCE-T Growth Inhibition Assay IC50=7.87783 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=7.99383 μM SANGER
COLO-684 Growth Inhibition Assay IC50=8.01818 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=8.07729 μM SANGER
TI-73 Growth Inhibition Assay IC50=8.25851 μM SANGER
BT-20 Growth Inhibition Assay IC50=8.26052 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=8.51834 μM SANGER
TE-12 Growth Inhibition Assay IC50=8.59931 μM SANGER
YH-13 Growth Inhibition Assay IC50=8.61008 μM SANGER
SF126 Growth Inhibition Assay IC50=8.83865 μM SANGER
J82 Growth Inhibition Assay IC50=8.90038 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=8.99561 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=9.04945 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=9.19137 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=9.1989 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=9.37657 μM SANGER
CTV-1 Growth Inhibition Assay IC50=9.56532 μM SANGER
HSC-2 Growth Inhibition Assay IC50=9.5755 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=9.61893 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=9.6875 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=9.75782 μM SANGER
HT-1080 Growth Inhibition Assay IC50=9.77739 μM SANGER
HEC-1 Growth Inhibition Assay IC50=10.3352 μM SANGER
AGS Growth Inhibition Assay IC50=10.374 μM SANGER
GAMG Growth Inhibition Assay IC50=10.5162 μM SANGER
SW48 Growth Inhibition Assay IC50=10.5189 μM SANGER
U031 Growth Inhibition Assay IC50=10.5908 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=10.6429 μM SANGER
SF295 Growth Inhibition Assay IC50=10.6704 μM SANGER
BHT-101 Growth Inhibition Assay IC50=10.7177 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=11.3201 μM SANGER
ACHN Growth Inhibition Assay IC50=11.4211 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=11.5043 μM SANGER
MN-60 Growth Inhibition Assay IC50=11.539 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=11.5466 μM SANGER
SCC-25 Growth Inhibition Assay IC50=11.7556 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=11.7637 μM SANGER
SN12C Growth Inhibition Assay IC50=11.9355 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=12.4234 μM SANGER
ME-180 Growth Inhibition Assay IC50=12.7054 μM SANGER
MC-IXC Growth Inhibition Assay IC50=12.7518 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=12.7614 μM SANGER
M059J Growth Inhibition Assay IC50=12.7727 μM SANGER
A2058 Growth Inhibition Assay IC50=12.8681 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=12.8785 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=12.9451 μM SANGER
KNS-42 Growth Inhibition Assay IC50=12.9984 μM SANGER
LoVo Growth Inhibition Assay IC50=13.2313 μM SANGER
AM-38 Growth Inhibition Assay IC50=13.2566 μM SANGER
NB5 Growth Inhibition Assay IC50=13.3752 μM SANGER
L-363 Growth Inhibition Assay IC50=13.4033 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=14.0645 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=14.6039 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=14.6077 μM SANGER
MFM-223 Growth Inhibition Assay IC50=15.1813 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=15.2767 μM SANGER
SW872 Growth Inhibition Assay IC50=15.3086 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=15.3306 μM SANGER
EW-1 Growth Inhibition Assay IC50=15.5462 μM SANGER
HN Growth Inhibition Assay IC50=15.5942 μM SANGER
SW837 Growth Inhibition Assay IC50=15.7847 μM SANGER
SCC-9 Growth Inhibition Assay IC50=15.8114 μM SANGER
MKN7 Growth Inhibition Assay IC50=15.9732 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=16.591 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=16.6116 μM SANGER
COR-L105 Growth Inhibition Assay IC50=16.6528 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=16.8389 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=16.8862 μM SANGER
TK10 Growth Inhibition Assay IC50=16.9473 μM SANGER
KNS-62 Growth Inhibition Assay IC50=16.9777 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=17.1732 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=17.2495 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=17.5219 μM SANGER
T-24 Growth Inhibition Assay IC50=17.5347 μM SANGER
HT-3 Growth Inhibition Assay IC50=17.5914 μM SANGER
KS-1 Growth Inhibition Assay IC50=17.673 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=17.798 μM SANGER
ABC-1 Growth Inhibition Assay IC50=17.8141 μM SANGER
BPH-1 Growth Inhibition Assay IC50=18.1685 μM SANGER
A431 Growth Inhibition Assay IC50=18.4127 μM SANGER
T98G Growth Inhibition Assay IC50=18.5157 μM SANGER
BHY Growth Inhibition Assay IC50=18.869 μM SANGER
Capan-2 Growth Inhibition Assay IC50=18.9078 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=18.9209 μM SANGER
CAL-27 Growth Inhibition Assay IC50=19.0487 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=19.8657 μM SANGER
KU812 Growth Inhibition Assay IC50=19.9573 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=20.001 μM SANGER
Mewo Growth Inhibition Assay IC50=20.1288 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=20.1477 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=20.2704 μM SANGER
EKVX Growth Inhibition Assay IC50=20.606 μM SANGER
RT-112 Growth Inhibition Assay IC50=20.6122 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=20.9803 μM SANGER
SW900 Growth Inhibition Assay IC50=21.0149 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=21.1277 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=21.1649 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=21.2745 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=21.3536 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=21.3692 μM SANGER
CTB-1 Growth Inhibition Assay IC50=21.4755 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=22.1582 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=22.5169 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=22.5555 μM SANGER
TE-8 Growth Inhibition Assay IC50=23.2565 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=25.3536 μM SANGER
COLO-680N Growth Inhibition Assay IC50=25.6329 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=25.644 μM SANGER
NB10 Growth Inhibition Assay IC50=26.3117 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=26.4713 μM SANGER
GMS-10 Growth Inhibition Assay IC50=26.8638 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=26.9998 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=27.0638 μM SANGER
DJM-1 Growth Inhibition Assay IC50=27.1454 μM SANGER
UACC-893 Growth Inhibition Assay IC50=27.9878 μM SANGER
C8166 Growth Inhibition Assay IC50=28.6938 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=28.6975 μM SANGER
TYK-nu Growth Inhibition Assay IC50=30.0345 μM SANGER
SW1710 Growth Inhibition Assay IC50=30.126 μM SANGER
A375 Growth Inhibition Assay IC50=30.3243 μM SANGER
HMV-II Growth Inhibition Assay IC50=31.3592 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=31.6352 μM SANGER
CAL-54 Growth Inhibition Assay IC50=31.7241 μM SANGER
HCC70 Growth Inhibition Assay IC50=32.1387 μM SANGER
ES1 Growth Inhibition Assay IC50=32.3062 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=33.204 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=33.2332 μM SANGER
MKN28 Growth Inhibition Assay IC50=33.3809 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=33.6931 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=34.1014 μM SANGER
SAS Growth Inhibition Assay IC50=34.4565 μM SANGER
HCC1395 Growth Inhibition Assay IC50=34.7186 μM SANGER
8305C Growth Inhibition Assay IC50=35.8415 μM SANGER
KM12 Growth Inhibition Assay IC50=36.7547 μM SANGER
SW1116 Growth Inhibition Assay IC50=37.5992 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=38.3389 μM SANGER
HCC2218 Growth Inhibition Assay IC50=38.6519 μM SANGER
T84 Growth Inhibition Assay IC50=38.7409 μM SANGER
ETK-1 Growth Inhibition Assay IC50=39.022 μM SANGER
COLO-800 Growth Inhibition Assay IC50=39.3868 μM SANGER
CAL-12T Growth Inhibition Assay IC50=39.5281 μM SANGER
ACN Growth Inhibition Assay IC50=40.4911 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=41.1596 μM SANGER
PSN1 Growth Inhibition Assay IC50=41.1749 μM SANGER
D-566MG Growth Inhibition Assay IC50=41.2086 μM SANGER
EGI-1 Growth Inhibition Assay IC50=42.428 μM SANGER
A204 Growth Inhibition Assay IC50=42.6388 μM SANGER
Saos-2 Growth Inhibition Assay IC50=42.8369 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=43.6878 μM SANGER
HLE Growth Inhibition Assay IC50=44.0856 μM SANGER
SW1463 Growth Inhibition Assay IC50=44.9971 μM SANGER
DSH1 Growth Inhibition Assay IC50=45.0033 μM SANGER
MCF7 Growth Inhibition Assay IC50=45.5051 μM SANGER
K5 Growth Inhibition Assay IC50=45.9405 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=47.215 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=47.2374 μM SANGER
SW948 Growth Inhibition Assay IC50=47.464 μM SANGER
BALL-1 Growth Inhibition Assay IC50=47.6168 μM SANGER
TE-9 Growth Inhibition Assay IC50=47.9581 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=48.0358 μM SANGER
KALS-1 Growth Inhibition Assay IC50=48.1289 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=48.7445 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=49.1152 μM SANGER
OC-314 Growth Inhibition Assay IC50=49.6834 μM SANGER
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 974.61 Formel

C47H55ClF3N5O6S3

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 923564-51-6 SDF herunterladen Lagerung von Stammlösungen

Synonyme N/A Smiles CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)NC(CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C

Löslichkeit

In vitro
Charge:

DMSO : 100 mg/mL (102.6 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

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
Bcl-xL
(Cell-free assay)
<=0.5 nM(Ki)
Bcl-2
(Cell-free assay)
<=1 nM(Ki)
Bcl-w
(Cell-free assay)
<=1 nM(Ki)
In vitro
Strukturell verwandt mit ABT-737, ist Navitoclax (ABT-263) ein Disruptor der Bcl-2/Bcl-xL-Interaktionen mit pro-apoptotischen Proteinen. Die Überexpression der Überlebens-Bcl-2-Familienmitglieder ist häufig mit Tumorerhalt, -progression und Chemoresistenz verbunden. Es zeigt den Schutz, der durch die Überexpression von Bcl-2 oder Bcl-xL geboten wird, mit EC50-Werten von 60 nM bzw. 20 nM. Eine breite Palette zellulärer Aktivitäten wird mit dieser Verbindung beobachtet, mit einer 50%igen Wachstumshemmung (EC50) von 110 nM gegen die empfindlichste Linie (H146), während ihre Aktivität in der am wenigsten empfindlichen Linie (H82) zu einem EC50 von 22 μM führt. Alle vier Zelllinien mit EC50-Werten von <400 nM (H146, H889, H1963 und H1417) sind auch hochsensitiv gegenüber ABT-737, und die beiden resistentesten Linien (H1048 und H82) sind ähnlich resistent gegenüber ABT-263.
Kinase-Assay
Affinitätsbestimmung
Die Bindungsaffinitäten (Ki oder IC50) von Navitoclax (ABT-263) gegen verschiedene Isoformen der Bcl-2-Familie werden mittels kompetitiver Fluoreszenzpolarisationsassays bestimmt. Es werden folgende Peptidprobe/Protein-Paare verwendet: f-bad (1 nM) und Bcl-xL (6 nM), f-Bax (1 nM) und Bcl-2 (10 nM), f-Bax (1 nM) und Bcl-w (40 nM), f-Noxa (2 nM) und Mcl-1 (40 nM), und f-Bax (1 nM) und Bcl-2-A1 (15 nM). Seine Bindungsaffinitäten für Bcl-xL werden auch unter Verwendung eines zeitaufgelösten Fluoreszenzresonanzenergietransfer-Assays bestimmt. Bcl-xL (1 nM, His-getaggt) wird mit 200 nM f-Bak, 1 nM Tb-markiertem Anti-His-Antikörper und dieser Verbindung bei Raumtemperatur für 30 Minuten gemischt. Die Fluoreszenz wird auf einem Envision-Plattenleser unter Verwendung eines 340/35 nm Anregungsfilters und 520/525 (f-Bak) und 495/510 nm (Tb-markierter Anti-His-Antikörper) Emissionsfiltern gemessen.
In vivo
Navitoclax (ABT-263) zeigt eine signifikante Antitumorwirksamkeit, wenn es in einer Dosis von 100 mg/kg/Tag im H345-Xenograftmodell verabreicht wird, mit 80% TGI und 20% der behandelten Tumoren, die mindestens eine 50%ige Reduktion des Tumorvolumens aufweisen. Die orale Verabreichung dieser Verbindung allein bewirkt vollständige Tumorregressionen in Xenograftmodellen von kleinzelligem Lungenkrebs und akuter lymphoblastischer Leukämie. In Xenograftmodellen von aggressivem B-Zell-Lymphom und multiplem Myelom, wo es eine moderate oder keine Einzelwirkstoffaktivität aufweist, verstärkt ABT-263 signifikant die Wirksamkeit klinisch relevanter Therapieschemata.
Literatur

Anwendungen

Methoden Biomarker Bilder PMID
Western blot STAT3 / pSTAT3 / STAT6 / pSTAT6 / Mcl-1 / Cleaved Mcl-1 / Bcl-xl / Bim / puma / Bik / Bax / PARP / c-Myc caspase3 / cleaved caspase 3
S1001-WB1
26811457
Growth inhibition assay Cell viability
S1001-viability1
25685063

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT05358639 Recruiting
High Grade Serous Carcinoma|Triple Negative Breast Cancer|Ovarian Cancer
Sunnybrook Health Sciences Centre|Exactis Innovation|Centre hospitalier de l''Université de Montréal (CHUM)|Princess Margaret Hospital Canada
 November 9 2022 Phase 1
NCT04480086 Terminated
Myelofibrosis (MF)
AbbVie
 March 17 2021 Phase 1
NCT04454658 Active not recruiting
Myelofibrosis (MF)
AbbVie
 November 11 2020 Phase 1

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Häufig gestellte Fragen

Frage 1:
Could you tell me if it can go through the hemato-encephalic barrier? This compound has the catalog number S1001.

Antwort:
According to the paper: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3223694/, it cannot cross the brain-blood barrier.