S81268 |
ABT-199 Venetoclax |
源叶(MedMol) | 99% |
- 产品描述:
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
- 靶点: Bcl-2:0.01 nM (Ki);Bcl-xL:48 nM (Ki);Bcl-W:245 nM (Ki);BCL; Autophagy
- 体内研究:
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.
- 参考文献:
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)
- 保存条件: -20℃
- 配置溶液浓度参考:
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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)