Navitoclax (ABT-263)
Navitoclax (ABT-263)是一种有效的Bcl-xL，Bcl-2和Bcl-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
CAS: 923564-51-6
产品质控
批次：
纯度：
99.99%
99.99
常与Navitoclax (ABT-263)一起在实验中被使用的化合物
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.
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.
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.
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。
Navitoclax (ABT-263)相关产品
相关信号通路图
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-xL，Bcl-2和Bcl-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 |
|
| 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 |
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 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
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
只
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，注：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：取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：取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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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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