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BMS-83 3923,Smoothened抑制剂

BMS-833923 （订货以英文为准）

编号：B126389
CAS号：1059734-66-5
分子式：C30H27N5O
分子量：473.57
货号 品牌 包装 目录价 您的价格 库存 数量 购买
B126389-50mg 阿拉丁 50mg ¥1853.90
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B126389-10mg 阿拉丁 10mg ¥583.90
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B126389-5mg 阿拉丁 5mg ¥346.90
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B126389-250mg 阿拉丁 250mg ¥4633.90
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产品名称 BMS-833923
中文名称 BMS-83 3923,Smoothened抑制剂
CAS号 1059734-66-5
分子式（M.F.） C30H27N5O
分子量（M.W.） 473.57
储存条件 -20°C储存
溶解性DMSO 95 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件储存温度-20°C
备注BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2.
生化机理Description:IC50 Value: 6-35 nM [1]BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity. SMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway.in vitro: In vitro, BMS-833923 inhibits the expression of downstream effectors in the HH pathway (GLI1 and PTCH1) in cell lines that express wild-type SMO and those which express activated mutant forms of SMO (IC50values of 6-35 nM). In FACS-based binding assays, BMS-833923 inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM [1].in vivo: Pharmacodynamic studies show that BMS-833923 robustly inhibits HH pathway activity with along duration of action after a single oral dose in medulloblastoma and pancreatic carcinoma xenograft models. The pharmacodynamic effects of BMS-833923 observed in these models translate into tumor growth inhibition at well-tolerated doses [1].Clinical trial: Dasatinib Combo With Smoothened (SMO) Antagonist (BMS-833923). Phase 2
别名XL139;Benzamide, N-[2-methyl-5-[(methylamino)methyl]phenyl]-4-[(4-phenyl-2-quinazolinyl)amino]-;XL139;Benzamide, N-[2-methyl-5-[(methylamino)methyl]phenyl]-4-[(4-phenyl-2-quinazolinyl)amino]-
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