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生物活性
ABT-737 is a novel and potent inhibitor of B-cell lymphoma 2 (BCL-2) family proteins, which are critical for cell survival and overexpressed in many tumor cells, with high affinity towards BCL-XL, BCL-2, and BCL-w but no affinity towards less homologous proteins, such as BCL-B, MCL-1, and A1. ABT-737 has shown single-agent activity against lymphoma and small-cell lung cancer as well as substantial antimyeloma activity both in vitro and in vivo. In recent studies, acute myeloid leukemia blast, origenitor, and stem cells are effectively killed by ABT-737 with normal hematopoietic cells intact. The disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway could also be induced by ABT-737.
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体外研究
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体内研究
30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)
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激酶实验
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细胞实验
0.001-10 μM
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动物实验
20 mg/kg和30 mg/kg 腹腔注射
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Konopleva M, et al. Cancer Cell, 2006, 10(5), 375-388.
[2] Kaiser, U., et al. 1996. Lung Cancer. 15: 31-40.
[3] Rudin, C.M., et al. 2004. J. Clin. Oncol. 22: 1110-1117.
[4] Trudel, S., et al. 2007. Clin. Cancer Res. 13: 621-629.
分子式
C42H45ClN6O5S2 |
分子量
813.43 |
CAS号
852808-04-9 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
|
DMSO
>150 mg/mL |
Water
<1 mg/mL |
Ethanol
<1 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
| NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
| NCT01440504 | Ovarian Cancer | Other: culture ex vivo with exposure to different therapeutic agents alone or in combination. | Centre Francois Baclesse|GRECAN | Phase 2 | 2010-04-01 | 2013-02-06 |
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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