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PF-5274857 Sale

目录号 : GC13280

PF-5274857 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-5274857 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。

PF-5274857 Chemical Structure

Cas No.:1373615-35-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,232.00
现货
5mg
¥1,120.00
现货
10mg
¥1,540.00
现货
50mg
¥6,300.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

PF-5274857 is an inhibitor of hedgehog (Hh) signaling pathway and is identified as a potent and selective antagonist of Smoothened (Smo) with an IC50 of 5.8 nM.

Smoothened, a G protein-coupled receptor, is a component of the hedgehog signaling pathway and is conserved from flies to humans. This protein is the molecular target of the teratogen cyclopamine. SMO can act as an oncogene and the activation of SMO mutations leads to unregulated activation of the hedgehog pathway and cancer.

In MEF cells, treatment of PF-5274857 completely blocked Shh-induced Hh pathway activity, which was measured by the transcriptional activity of Smo downstream gene Gli1.

In vivo, PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with IC50 of 8.9 nM. PF-5274857 also shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression. In skin tissue, downregulation of Gli1 and Gli2 is also observed with a similar time course by PF-52748571.

Reference:
1.   Rohner A, Spilker ME, Lam JL, et al. Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Molecular cancer therapeutics.2012;11(1):57-65.

Chemical Properties

Cas No. 1373615-35-0 SDF
化学名 1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one
Canonical SMILES CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CCS(=O)(=O)C)C
分子式 C20H25ClN4O3S 分子量 436.96
溶解度 ≥ 19.65mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2885 mL 11.4427 mL 22.8854 mL
5 mM 0.4577 mL 2.2885 mL 4.5771 mL
10 mM 0.2289 mL 1.1443 mL 2.2885 mL
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