PF-05274857 (hydrochloride) 是一种有效的、选择性的、具有口服活性的脑渗透性 Smo 拮抗剂，IC50 为 5.8 nM，Ki 为 4.6 nM。 PF-05274857（盐酸盐）具有研究肿瘤类型的潜力，包括由激活的 Hh 通路驱动的脑肿瘤和脑转移。
| Cas No. |
1613439-62-5 |
| Canonical SMILES |
ClC1=C(C2=NC=C(C)C=C2C)C=C(N3CCN(C(CCS(C)(=O)=O)=O)CC3)N=C1.Cl |
| 分子式 |
C20H25ClN4O3S.HCl |
| 分子量 |
473.4 |
| 溶解度 |
Soluble in DMSO |
| 储存条件 |
Store at -20°C |
| General tips |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition |
Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 半岛bd体育手机客户端 描述 |
Sonic hedgehog (Shh) signaling is initiated by binding of the ligand, Shh, to the receptor Patched 1, which relieves suppression by the associated receptor Smoothened (Smo). PF-05274857 is an antagonist which binds Smo (Ki = 4.6 nM), blocking Gli1 transcription in cells stimulated with Shh (IC50 = 2.7 nM). When administered orally, it distributes through plasma to skin and tumor and remains metabolically stable. PF-05274857 also penetrates the blood-brain barrier and inhibits Smo activity in the brain. |
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