Navitoclax (ABT-263)

Navitoclax (ABT-263)是一种有效的Bcl-xLBcl-2Bcl-w抑制剂,无细胞试验中Ki分别为≤0.5 nM,≤1 nM和≤1 nM,但与Mcl-1和A1结合微弱。Phase 2。

Navitoclax (ABT-263) Chemical Structure

Navitoclax (ABT-263) Chemical Structure

CAS: 923564-51-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
5mg RMB 647.01 现货
25mg RMB 1941.03 现货
100mg RMB 4823.91 现货
1g RMB 12039.3 现货
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客户使用Selleck的Navitoclax (ABT-263)发表文献341

产品质控

批次: 纯度: 99.99%
99.82

常与Navitoclax (ABT-263)一起在实验中被使用的化合物

A-1331852


Navitoclax和A-1331852选择性诱导衰老内皮细胞(ECs)凋亡。


Abdelgawad IY, et al. Biochim Biophys Acta Mol Basis Dis. 2022;1868(4):166352.

Venetoclax (ABT-199)


Venetoclax联合Navitoclax和化疗对复发/难治性急性淋巴细胞白血病患者具有良好的耐受性和良好的疗效。


Pullarkat VA, et al. Cancer Discov. 2021 Jun;11(6):1440-1453.

ABT-737


Navitoclax和ABT-737通过药理抑制BCL-XL诱导BAK/ bax介导的血小板凋亡。


Debrincat MA, et al. Cell Death Dis. 2015 Apr 16;6(4):e1721.

MG132


Navitoclax和MG132,联合GX15-070部分恢复了LN229胶质母细胞瘤细胞中蛋白BAG3和去泛素酶Usp9X的表达。


Karpel-Massler G, et al. Oncotarget. 2015;6(16):14507-14521.

Y-27632 2HCl


Navitoclax和Y-27632 2HCl协同增强线粒体启动,为硬皮病成纤维细胞凋亡提供了潜在的治疗策略。


Lagares D, et al. Sci Transl Med. 2017;9(420):eaal3765.

Navitoclax (ABT-263)相关产品

相关信号通路图

Bcl-2抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
NCI-H146 Cytotoxicity assay 48 h EC50 = 0.0867 μM 18841882
FDC-P1 BCL-xL inhibition assay 24 h IC50 = 0.06 μM 24881567
NCI-H1417 Cytotoxicity assay 4 days IC50 = 0.0542 μM 23448298
NCI-H187 Cytotoxicity assay 4 days IC50 = 0.0384 μM 23448298
NCI-H1963 Cytotoxicity assay 4 days IC50 = 0.0266 μM 23448298
FDC-P1 BCL-2 inhibition assay 24 h IC50 = 0.015 μM 24881567
RS4:11 Apoptosis assay 6 h EC50 = 0.014 μM 24881567
FL5.12 Cytotoxicity assay 24 h EC50 = 0.0059 μM 18841882
FL5.12 Cytotoxicity assay 24 h EC50 = 0.0042 μM 18841882
KARPAS-299 Growth Inhibition Assay IC50=3.67361 μM SANGER
H9 Growth Inhibition Assay IC50=3.67144 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=3.63472 μM SANGER
5637 Growth Inhibition Assay IC50=3.61103 μM SANGER
RVH-421 Growth Inhibition Assay IC50=3.56877 μM SANGER
EFM-19 Growth Inhibition Assay IC50=3.48339 μM SANGER
AN3-CA Growth Inhibition Assay IC50=3.44238 μM SANGER
NBsusSR Growth Inhibition Assay IC50=3.34938 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=3.31272 μM SANGER
SW626 Growth Inhibition Assay IC50=3.24543 μM SANGER
GCIY Growth Inhibition Assay IC50=3.20491 μM SANGER
MPP-89 Growth Inhibition Assay IC50=3.05666 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=3.04997 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=3.01417 μM SANGER
U-118-MG Growth Inhibition Assay IC50=2.96491 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=2.82782 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=2.79681 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=2.72215 μM SANGER
GOTO Growth Inhibition Assay IC50=2.65377 μM SANGER
IGR-1 Growth Inhibition Assay IC50=2.62035 μM SANGER
HOP-92 Growth Inhibition Assay IC50=2.58743 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=2.57681 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=2.51158 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=2.4878 μM SANGER
TE-11 Growth Inhibition Assay IC50=2.29473 μM SANGER
ES8 Growth Inhibition Assay IC50=2.25471 μM SANGER
MFE-280 Growth Inhibition Assay IC50=2.02848 μM SANGER
RCM-1 Growth Inhibition Assay IC50=2.00399 μM SANGER
MLMA Growth Inhibition Assay IC50=1.96677 μM SANGER
HSC-3 Growth Inhibition Assay IC50=1.96365 μM SANGER
EW-11 Growth Inhibition Assay IC50=1.95657 μM SANGER
OMC-1 Growth Inhibition Assay IC50=1.86016 μM SANGER
COR-L23 Growth Inhibition Assay IC50=1.79874 μM SANGER
SNU-423 Growth Inhibition Assay IC50=1.78157 μM SANGER
DEL Growth Inhibition Assay IC50=1.74692 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=1.73656 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=1.72201 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=1.71418 μM SANGER
Calu-3 Growth Inhibition Assay IC50=1.70697 μM SANGER
A388 Growth Inhibition Assay IC50=1.68724 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.67293 μM SANGER
SCC-4 Growth Inhibition Assay IC50=1.59887 μM SANGER
D-247MG Growth Inhibition Assay IC50=1.51122 μM SANGER
NB69 Growth Inhibition Assay IC50=1.46271 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=1.40269 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=1.3885 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=1.36555 μM SANGER
ES4 Growth Inhibition Assay IC50=1.34998 μM SANGER
HEL Growth Inhibition Assay IC50=1.31029 μM SANGER
ES7 Growth Inhibition Assay IC50=1.27951 μM SANGER
COLO-792 Growth Inhibition Assay IC50=1.20071 μM SANGER
HCC2157 Growth Inhibition Assay IC50=1.19494 μM SANGER
C32 Growth Inhibition Assay IC50=1.19088 μM SANGER
SBC-1 Growth Inhibition Assay IC50=1.19053 μM SANGER
CAL-120 Growth Inhibition Assay IC50=1.16429 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=1.16236 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=1.14152 μM SANGER
NB14 Growth Inhibition Assay IC50=1.13748 μM SANGER
HCC2998 Growth Inhibition Assay IC50=1.07135 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=1.0623 μM SANGER
P30-OHK Growth Inhibition Assay IC50=1.04688 μM SANGER
COLO-824 Growth Inhibition Assay IC50=1.01708 μM SANGER
L-428 Growth Inhibition Assay IC50=1.0125 μM SANGER
OAW-42 Growth Inhibition Assay IC50=0.96146 μM SANGER
PA-1 Growth Inhibition Assay IC50=0.95642 μM SANGER
A427 Growth Inhibition Assay IC50=0.93022 μM SANGER
HPAF-II Growth Inhibition Assay IC50=0.92628 μM SANGER
DU-145 Growth Inhibition Assay IC50=0.89923 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.81328 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=0.81121 μM SANGER
HCC38 Growth Inhibition Assay IC50=0.8019 μM SANGER
OAW-28 Growth Inhibition Assay IC50=0.7837 μM SANGER
RD Growth Inhibition Assay IC50=0.75899 μM SANGER
HAL-01 Growth Inhibition Assay IC50=0.72549 μM SANGER
DU-4475 Growth Inhibition Assay IC50=0.65427 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.65264 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.60808 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.59207 μM SANGER
EW-13 Growth Inhibition Assay IC50=0.58341 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.5832 μM SANGER
DB Growth Inhibition Assay IC50=0.5708 μM SANGER
SW1417 Growth Inhibition Assay IC50=0.55438 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=0.50953 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.50019 μM SANGER
RMG-I Growth Inhibition Assay IC50=0.49464 μM SANGER
MS-1 Growth Inhibition Assay IC50=0.46933 μM SANGER
EW-22 Growth Inhibition Assay IC50=0.46671 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.46613 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=0.46157 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=0.45778 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=0.45652 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=0.44017 μM SANGER
A704 Growth Inhibition Assay IC50=0.4267 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=0.41023 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.3654 μM SANGER
BE-13 Growth Inhibition Assay IC50=0.36459 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=0.35343 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=0.33529 μM SANGER
WM-115 Growth Inhibition Assay IC50=0.27738 μM SANGER
HuO9 Growth Inhibition Assay IC50=0.26715 μM SANGER
HCC1569 Growth Inhibition Assay IC50=0.25106 μM SANGER
BEN Growth Inhibition Assay IC50=0.23968 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=0.23573 μM SANGER
NB12 Growth Inhibition Assay IC50=0.23115 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.21988 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.20498 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.19918 μM SANGER
LU-134-A Growth Inhibition Assay IC50=0.18671 μM SANGER
LU-135 Growth Inhibition Assay IC50=0.18552 μM SANGER
D-283MED Growth Inhibition Assay IC50=0.17686 μM SANGER
CHP-134 Growth Inhibition Assay IC50=0.16306 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=0.15169 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.1137 μM SANGER
697 Growth Inhibition Assay IC50=0.10839 μM SANGER
NH-12 Growth Inhibition Assay IC50=0.10744 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=0.10275 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.08704 μM SANGER
NB13 Growth Inhibition Assay IC50=0.08203 μM SANGER
EW-3 Growth Inhibition Assay IC50=0.08053 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.07815 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=0.07778 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.07213 μM SANGER
NB17 Growth Inhibition Assay IC50=0.07124 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.06841 μM SANGER
RH-18 Growth Inhibition Assay IC50=0.06048 μM SANGER
ATN-1 Growth Inhibition Assay IC50=0.04733 μM SANGER
TGW Growth Inhibition Assay IC50=0.04633 μM SANGER
KG-1 Growth Inhibition Assay IC50=0.04486 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=0.04287 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.04011 μM SANGER
ECC10 Growth Inhibition Assay IC50=0.03792 μM SANGER
KY821 Growth Inhibition Assay IC50=0.02975 μM SANGER
HL-60 Growth Inhibition Assay IC50=0.02908 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.02587 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.02314 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.01983 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.01699 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=0.01586 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.00669 μM SANGER
MOLT4 Antiproliferative activity assay EC50 = 0.303 μM 28926247
RS4:11 Antiproliferative activity assay EC50 = 0.112 μM 28926247
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
点击查看更多细胞系数据

生物活性

产品描述 Navitoclax (ABT-263)是一种有效的Bcl-xLBcl-2Bcl-w抑制剂,无细胞试验中Ki分别为≤0.5 nM,≤1 nM和≤1 nM,但与Mcl-1和A1结合微弱。Phase 2。
靶点
Bcl-xL [1]
(Cell-free assay)
Bcl-2 [1]
(Cell-free assay)
Bcl-w [1]
(Cell-free assay)
<=0.5 nM(Ki) <=1 nM(Ki) <=1 nM(Ki)
体外研究(In Vitro)
体外研究活性 ABT-263有效抑制Bcl-2蛋白家族,用荧光偏振分析法测试ABT-263作用于Bcl-xL, Bcl-2和 Bcl-w时,Ki分别为0.5, 1和1 nM。[1]ABT-263结构上与ABT-737相关。ABT-263阻断Bcl-2 和Bcl-XL与凋亡前体蛋白相互作用。Bcl-2家族成员Bcl-2,Bcl-XL, 和Mcl-1的过量表达通常都与肿瘤的修复及抗药性有关。ABT-263作用于过量表达的Bcl-2 和Bcl-XL时显示出保护作用,EC50分别为60 和20 nM。ABT-263作用于不同的细胞显示出不同的细胞活性,作用于H146细胞系时EC50为110nM,而作用于H82细胞系时EC50为22 µM。ABT-737可以有效作用于四种EC50值 <400 nM的细胞系,即H146, H889, H1963, 和H1417。而两种抗ABT-737的细胞系,即H1048和H82,同样也显示出抗ABT-263的特性。[2]
激酶实验 激酶实验
用竞争性荧光偏振检测测定ABT-263 作用于Bcl-2 家族不同亚型的Ki值或者IC50值。使用如下的肽探针对或者蛋白对:f-bad (1 nM) 和Bcl-xL (6 nM), f-Bax (1 nM) 和Bcl-2 (10 nM), f-Bax (1 nM) 和Bcl-w (40 nM), f-Noxa (2 nM)和Mcl-1 (40 nM), 及f-Bax (1 nM) 和Bcl-2-A1 (15 nM)。用时间分辨荧光共振能转移法测定ABT-263和Bcl-xL作用的结合紧密度。1 nM 用His标记的Bcl-xL 与200 nM f-Bak,及 1 nM Tb标记的His抗体混合, 然后在室温下处理30分钟。
实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性 用ABT-263处理H345移植瘤模型,按动物体重,每千克每天处理10mg ABT-263,结果肿瘤生长抑制率达80% ,肿瘤体积减小了50%以上,显示出ABT-263极强的抗癌效果。ABT-263作用于非小细胞肺癌和急性淋巴细胞白血病的移植瘤模型时,每天单独口服,结果显示肿瘤完全衰退。ABT-263单独作用于B-细胞淋巴瘤和多发性骨髓瘤的移植瘤模型时效果不明显,但是可以显著增强临床其他相关用药的药性。[2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date 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

化学信息&溶解度

分子量 974.61 分子式

C47H55ClF3N5O6S3

CAS号 923564-51-6 SDF Download Navitoclax (ABT-263) SDF
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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 102.6 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

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常见问题及建议解决方法

问题 1:
Could you tell me if the catalog number S1001 can go through the hemato-encephalic barrier?

回答:
According to the paper: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3223694/, ABT-263 can not cross brain-blood barrier.

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