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Navitoclax (ABT-263)
Navitoclax (ABT-263)是一種有效的Bcl-xL，Bcl-2和Bcl-w抑制劑，無細胞試驗中Ki分別為≤0.5 nM，≤1 nM和≤1 nM，但與Mcl-1和A1結(jié)合微弱。Phase 2。
Navitoclax (ABT-263) Chemical Structure
CAS: 923564-51-6
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
常與Navitoclax (ABT-263)一起在實驗中被使用的化合物
Navitoclax和A-1331852選擇性誘導(dǎo)衰老內(nèi)皮細胞(ECs)凋亡。
Abdelgawad IY, et al. Biochim Biophys Acta Mol Basis Dis. 2022;1868(4):166352.
Venetoclax聯(lián)合Navitoclax和化療對復(fù)發(fā)/難治性急性淋巴細胞白血病患者具有良好的耐受性和良好的療效。
Pullarkat VA, et al. Cancer Discov. 2021 Jun;11(6):1440-1453.
Navitoclax和ABT-737通過藥理抑制BCL-XL誘導(dǎo)BAK/ bax介導(dǎo)的血小板凋亡。
Debrincat MA, et al. Cell Death Dis. 2015 Apr 16;6(4):e1721.
Navitoclax和MG132，聯(lián)合GX15-070部分恢復(fù)了LN229膠質(zhì)母細胞瘤細胞中蛋白BAG3和去泛素酶Usp9X的表達。
Karpel-Massler G, et al. Oncotarget. 2015;6(16):14507-14521.
Navitoclax和Y-27632 2HCl協(xié)同增強線粒體啟動，為硬皮病成纖維細胞凋亡提供了潛在的治療策略。
Navitoclax (ABT-263)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Navitoclax (ABT-263)是一種有效的Bcl-xL，Bcl-2和Bcl-w抑制劑，無細胞試驗中Ki分別為≤0.5 nM，≤1 nM和≤1 nM，但與Mcl-1和A1結(jié)合微弱。Phase 2。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | ABT-263有效抑制Bcl-2蛋白家族，用熒光偏振分析法測試ABT-263作用于Bcl-xL, Bcl-2和 Bcl-w時，Ki分別為0.5, 1和1 nM。[1]ABT-263結(jié)構(gòu)上與ABT-737相關(guān)。ABT-263阻斷Bcl-2 和Bcl-XL與凋亡前體蛋白相互作用。Bcl-2家族成員Bcl-2,Bcl-XL, 和Mcl-1的過量表達通常都與腫瘤的修復(fù)及抗藥性有關(guān)。ABT-263作用于過量表達的Bcl-2 和Bcl-XL時顯示出保護作用，EC50分別為60 和20 nM。ABT-263作用于不同的細胞顯示出不同的細胞活性，作用于H146細胞系時EC50為110nM,而作用于H82細胞系時EC50為22 μM。ABT-737可以有效作用于四種EC50值 <400 nM的細胞系，即H146, H889, H1963, 和H1417。而兩種抗ABT-737的細胞系，即H1048和H82，同樣也顯示出抗ABT-263的特性。[2] | |||
|---|---|---|---|---|
| 激酶實驗 | 激酶實驗 | |||
| 用競爭性熒光偏振檢測測定ABT-263 作用于Bcl-2 家族不同亞型的Ki值或者IC50值。使用如下的肽探針對或者蛋白對：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)。用時間分辨熒光共振能轉(zhuǎn)移法測定ABT-263和Bcl-xL作用的結(jié)合緊密度。1 nM 用His標記的Bcl-xL 與200 nM f-Bak,及 1 nM Tb標記的His抗體混合, 然后在室溫下處理30分鐘。 | ||||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 用ABT-263處理H345移植瘤模型，按動物體重，每千克每天處理10mg ABT-263，結(jié)果腫瘤生長抑制率達80% ，腫瘤體積減小了50%以上，顯示出ABT-263極強的抗癌效果。ABT-263作用于非小細胞肺癌和急性淋巴細胞白血病的移植瘤模型時，每天單獨口服，結(jié)果顯示腫瘤完全衰退。ABT-263單獨作用于B-細胞淋巴瘤和多發(fā)性骨髓瘤的移植瘤模型時效果不明顯，但是可以顯著增強臨床其他相關(guān)用藥的藥性。[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 |
化學(xué)信息&溶解度
| 分子量 | 974.61 | 分子式 | C47H55ClF3N5O6S3 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (102.6 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
常見問題及建議解決方法
問題 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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