常用名 | 3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺 | CAS号 | 728033-96-3 |
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价格 | 纯度 | 98.0% | |
备货期 | 10天 | 库存 | 现货 |
产品详情(用途,包装等)
用途: OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kit activated) [1]Target: VEGFR2/Kit/CSF1Rin vitro: OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM [1]. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode [2].in vivo: OSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models [1]. 物理化学性质: CAS号:728033-96-3 常用中文名:3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺 常用英文名:OSI-930 分子式:C22H16F3N3O2S 分子量:443.441 密度:1.5±0.1 g/cm3 沸点:517.4±50.0 °C at 760 mmHg 熔点:N/A 闪点:266.7±30.1 °C 储存条件:-20℃ |