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Navitoclax (ABT-263) Bcl-2 inhibiteur

Name: Navitoclax (ABT-263)
Brand: Selleck Chemicals
SKU: S1001
Rating: 5 (399 reviews)

N° Cat.S1001

Puissant inhibiteur de Bcl-xL, Bcl-2 et Bcl-w avec un K_i de ≤ 0,5 nM, ≤1 nM et ≤1 nM dans les essais sans cellules, Navitoclax (ABT-263) se lie plus faiblement à Mcl-1 et A1. Phase 2.

Navitoclax (ABT-263) Bcl-2 inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 974.61

Aller à

Contrôle qualité

Lot : Pureté : 99.86%

99.86

Produits Souvent Utilisés Avec 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.

Cibles apparentées	Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Autre Bcl-2 Inhibiteurs	S63845 Obatoclax Mesylate (GX15-070) A-1210477 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77 (R)-(-)-Gossypol (AT-101) acetic acid A-1155463 Sabutoclax

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Temps dincubation	Description de lactivité	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
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire	974.61	Formule	C₄₇H₅₅ClF₃N₅O₆S₃	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	923564-51-6	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	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

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (102.6 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	0.800mg/ml (0.82mM)	Taking the 1 mL working solution as an example, add 20 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	4.000mg/ml (4.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.000mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.000mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.550mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 31 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

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	Structurellement apparenté à l'ABT-737, Navitoclax (ABT-263) est un perturbateur des interactions Bcl-2/Bcl-xL avec les protéines pro-apoptotiques. La surexpression des membres de la famille Bcl-2 favorisant la survie est fréquemment associée au maintien, à la progression et à la chimiorésistance des tumeurs. Il présente la protection conférée par la surexpression de Bcl-2 ou Bcl-xL avec des valeurs EC50 de 60 nM et 20 nM, respectivement. Un large éventail d'activités cellulaires est observé avec ce composé, ayant une inhibition de croissance de 50 % (EC50) de 110 nM contre la lignée la plus sensible (H146), tandis que son activité dans la lignée la moins sensible (H82) entraîne un EC50 à 22 μM. Les quatre lignées cellulaires avec des valeurs EC50 de <400 nM (H146, H889, H1963 et H1417) sont également très sensibles à l'ABT-737, et les deux lignées les plus résistantes (H1048 et H82) sont également résistantes à l'ABT-263.
Kinase Assay	Détermination de l'affinité
Kinase Assay	Les affinités de liaison (K_i ou IC50) de Navitoclax (ABT-263) contre différentes isoformes de la famille Bcl-2 sont déterminées par des essais de polarisation de fluorescence compétitifs. Les paires sonde peptidique/protéine suivantes sont utilisées : f-bad (1 nM) et Bcl-xL (6 nM), f-Bax (1 nM) et Bcl-2 (10 nM), f-Bax (1 nM) et Bcl-w (40 nM), f-Noxa (2 nM) et Mcl-1 (40 nM), et f-Bax (1 nM) et Bcl-2-A1 (15 nM). Ses affinités de liaison pour Bcl-xL sont également déterminées à l'aide d'un essai de transfert d'énergie de résonance par fluorescence résolue dans le temps. Bcl-xL (1 nM, marqué His) est mélangé avec 200 nM de f-Bak, 1 nM d'anticorps anti-His marqué Tb, et ce composé à température ambiante pendant 30 min. La fluorescence est mesurée sur un lecteur de plaques Envision à l'aide d'un filtre d'excitation de 340/35 nm et de filtres d'émission de 520/525 (f-Bak) et 495/510 nm (anticorps anti-His marqué Tb).
In vivo	Navitoclax (ABT-263) démontre une efficacité antitumorale significative lorsqu'il est administré à 100 mg/kg/jour dans le modèle de xénogreffe H345, avec 80 % de TGI et 20 % des tumeurs traitées indiquant au moins une réduction de 50 % du volume tumoral. L'administration orale de ce composé seul provoque des régressions tumorales complètes dans les modèles de xénogreffe de cancer du poumon à petites cellules et de leucémie lymphoblastique aiguë. Dans les modèles de xénogreffe de lymphome à cellules B agressif et de myélome multiple où il affiche une activité modeste ou nulle en monothérapie, ABT-263 améliore significativement l'efficacité des régimes thérapeutiques cliniquement pertinents.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18451170/ [2] https://pubmed.ncbi.nlm.nih.gov/18519752/

Applications

Méthodes	Biomarqueurs	Images	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		26811457
Growth inhibition assay	Cell viability		25685063

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
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

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Questions fréquemment posées

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

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

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