- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
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Navitoclax (ABT-263)
ナビトクラックス (Navitoclax (ABT-263)) は Bcl-xL, Bcl-2 and Bcl-w の強力な阻害剤であり、阻害定数は cell-free assay において Ki ≦ 0.5 nM, 1 nM および 1nM です。一方、Mcl-1 および A1 に対しては比較的弱い結合力を示します。臨床第2相試験中
CAS No. 923564-51-6
文献中Selleckの製品使用例（365）
製品安全説明書
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Navitoclax (ABT-263)と併用されることが多い化合物
Navitoclax and A-1331852 selectively induce apoptosis in senescent endothelial cells (ECs).
Abdelgawad IY, et al. Biochim Biophys Acta Mol Basis Dis. 2022;1868(4):166352.
Navitoclax and ABT-737 induce BAK/BAX-mediated platelet apoptosis by pharmacologically suppressing BCL-XL.
Debrincat MA, et al. Cell Death Dis. 2015 Apr 16;6(4):e1721.
Navitoclax 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.
Karpel-Massler G, et al. Oncotarget. 2015;6(16):14507-14521.
Navitoclax and Y-27632 2HCl synergistically enhance mitochondrial priming and provide a potential therapeutic strategy for scleroderma fibroblast apoptosis.
Navitoclax (ABT-263)関連製品
シグナル伝達経路
Bcl-2阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| 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 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | ナビトクラックス (Navitoclax (ABT-263)) は Bcl-xL, Bcl-2 and Bcl-w の強力な阻害剤であり、阻害定数は cell-free assay において Ki ≦ 0.5 nM, 1 nM および 1nM です。一方、Mcl-1 および A1 に対しては比較的弱い結合力を示します。臨床第2相試験中 | ||||||
|---|---|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. Overexpression of the prosurvival Bcl-2 family members is commonly associated with tumor maintenance, progression, and chemoresistance. [1] ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. [1] A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263. [2] | |||
|---|---|---|---|---|
| Kinase Assay | Affinity determination | |||
| Binding affinities (Ki or IC50) of ABT-263 against different isoforms of Bcl-2 family are determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs are used: f-bad (1 nM) and Bcl-xL (6 nM), f-Bax (1 nM) and Bcl-2 (10 nM), f-Bax (1 nM) and Bcl-w (40 nM), f-Noxa (2 nM) and Mcl-1 (40 nM), and f-Bax (1 nM) and Bcl-2-A1 (15 nM). Binding affinities for Bcl-xL are also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nM, His tagged) is mixed with 200 nM f-Bak, 1 nM Tb-labeled anti-His antibody, and ABT-263 at room temperature for 30 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters. | ||||
| 細胞実験 | 細胞株 | SCLC cell lines | ||
| 濃度 | 0-1 μM | |||
| 反応時間 | 48 hours | |||
| 実験の流れ | Human tumor cell lines SCLC cell lines are maintained at 37℃ containing 5% CO2. SCLC cell lines are cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mM HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines are cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1-5×10 4) are treated by ABT-263 for 48 hours in 96-well culture plates in a final volume of 100 μL and cytotoxicity is assessed with the CellTiter Glo assay. In vitro cyto toxicity of ABT-263 is assayed. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | 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 | |
| In Vivo | ||
| In Vivo | When ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. [2] Oral administration of ABT-263 alone causes complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia. In xenograft models of aggressive B-cell lymphoma and multiple myeloma where ABT-263 displays modest or no single agent activity, it significantly enhances the efficacy of clinically relevant therapeutic regimens. [2] | |
|---|---|---|
| 動物実験 | 動物モデル | C.B.-17 scid-bg or C.B.-17 scid mice |
| 投与量 | 100 mg/kg/d | |
| 投与経路 | Administered via p.o. | |
| 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 |
化学情報
| 分子量 | 974.61 | 化学式 | C47H55ClF3N5O6S3 |
| CAS No. | 923564-51-6 | SDF | Download Navitoclax (ABT-263) SDFをダウンロードする |
| 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 | ||
| 保管 | |||
|
In vitro |
DMSO : 100 mg/mL ( (102.6 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問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.
Tags: Navitoclax (ABT-263)を買う | Navitoclax (ABT-263) ic50 | Navitoclax (ABT-263)供給者 | Navitoclax (ABT-263)を購入する | Navitoclax (ABT-263)費用 | Navitoclax (ABT-263)生産者 | オーダーNavitoclax (ABT-263) | Navitoclax (ABT-263)化学構造 | Navitoclax (ABT-263)分子量 | Navitoclax (ABT-263)代理店
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