| 產(chǎn)品描述： | Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy |
| 靶點(diǎn)： |
Bcl-2：0.01 nM (Ki)；Bcl-xL：48 nM (Ki)；Bcl-W：245 nM (Ki);BCL;?Autophagy |
| 體內(nèi)研究： |
After a single oral dose of 12.5 mg per kg body weight in xenografts derived from RS4;11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05). Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with Venetoclax (ABT-199) 100 mg/kg for 4 days results in a significant reduction of leukemic burden. |
| 參考文獻(xiàn)： |
1. Souers AJ, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8. 2. Peirs S, et al. ABT-199 mediated inhibition of BCL-2 as a novel therapeutic strategy in T-cell acute lymphoblastic leukemia. Blood. 2014 Dec 11;124(25):3738-47. 3. Bi C, et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764. |
| 溶解性： |
DMSO : 77.5 mg/mL (89.24 mM; Need ultrasonic) Ethanol : < 1 mg/mL (insoluble) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.151 ml |
5.757 ml |
11.515 ml |
| 5 mM |
0.23 ml |
1.151 ml |
2.303 ml |
| 10 mM |
0.115 ml |
0.576 ml |
1.151 ml |
| 50 mM |
0.023 ml |
0.115 ml |
0.23 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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