产品名称

英文名称：PF-5274857

同义词

PF-5274857、1373615-35-0、1-(4-(5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one、PF-5274857 freebase、1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one、1-(4-(5

产品性质

CAS编号：1373615-35-0

分子式：C20H25ClN4O3S

分子量：436.96

PubChem编号：56956240

英文别名：PF-5274857|1373615-35-0|1-(4-(5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one|PF-5274857 freebase|1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one|1-(4-(5

规格或纯度：98%

英文名称：PF-5274857

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.PF-5274857 is a hedgehog (Hh) signaling pathway inhibitor acting as a potent and selective Smoothened (Smo) antagonist with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 completely blocked downstream gene Gli1 transcriptional activity in Gli-Luc mouse embryonic fibroblast (MEF) cells with an IC50 of 2.7 nM. PF-5274857 is brain penetrant. The compound PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with an in vivo IC50 of 8.9 nM.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍PF-5274857是hedgehog (Hh)信号通路的抑制剂，作为Smoothened (Smo)的高效选择性拮抗剂，其IC50值为5.8 nM。作为G蛋白偶联受体，Smoothened是hedgehog信号通路的组分，从果蝇到人类皆保守。此蛋白是致畸环巴胺的分子靶点。SMO可以作为原癌基因，SMO激活突变导致hedgehog信号通路不受控制的活化和癌症。通过检测Smo下游基因Gli的转录活性可知，PF-5274857处理MEF细胞能够完全抑制Shh诱导的Hh信号通路活性。PF-5274857是一种有效的，选择性Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，IC50和Ki分别为5.8 nM和4.6 nM，可以穿透血脑屏障。

IUPAC Name：1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one

INCHI：InChI=1S/C20H25ClN4O3S/c1-14-10-15(2)20(23-12-14)16-11-18(22-13-17(16)21)24-5-7-25(8-6-24)19(26)4-9-29(3,27)28/h10-13H,4-9H2,1-3H3

InChi Key：BBVNTTZIOTWDSV-UHFFFAOYSA-N

Canonical SMILES：CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CCS(=O)(=O)C)C

Isomeric SMILES：CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CCS(=O)(=O)C)C

PubChem CID：56956240

溶解性：DMSO 93 mg/mL Water 93 mg/mL Ethanol <1 mg/mL

产品包装