| 溶解性 | DMSO 93 mg/mL Water 93 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 备注 | PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier. |
| 生化机理 | PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ± 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ± 1.4 nmol/L in cells. This Smo antagonist PF-5274857 showed robust antitumor activity in a mouse model of medulloblastoma with an in vivo IC(50) of 8.9 ± 2.6 nmol/L. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hedgehog (Hh) signaling pathway. |
| 别名 | 1-(4-(5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one;1-(4-(5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one |
PF-5274857
PF-5274857 （订货以英文为准）
编号：P126554
CAS号：1373615-35-0
分子式：C20H25CLN4O3S
分子量：436.96
| 产品名称 | PF-5274857 |
| 中文名称 | PF-5274857 |
| CAS号 | 1373615-35-0 |
| 分子式（M.F.） | C20H25CLN4O3S |
| 分子量（M.W.） | 436.96 |
| 储存条件 | -20°C储存 |
| 标识符号 | https://www.aladdin-e.com/images/ghs/ghs07.jpg |
| 信号词 | Warning |
| 危害声明 | H315,H319,H335 |
| 警示性声明 | P261,P305+P351+P338 |
| WGK德国 | 3 |
| 风险声明 (欧洲) | 36/37/38 |
| 安全声明（欧洲） | 26 |
| 危害码（欧洲） | Xi |
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