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PF-5274857 hydrochloride,≥98% (HPLC)

别名:PF5274857盐酸盐;1-[4-(5′-Chloro-3,5-dimethyl-2,4′-bipyridin-2′-yl)piperazin-1-yl] -3- (methylsulfonyl)propan-1-one hydrochloride;1-[4-(5'-氯-3,5-二甲基[2,4'-联吡啶]-2'-基)-1-哌嗪基]-3-(甲基磺酰基)-1-丙酮

Empirical Formula (Hill Notation): C20H25ClN4O3S · HCl CAS号: 1373615-35-0 (free base) 分子量: 473.42 MDL编号: MFCD24387542 PubChem化学物质编号: 329823776 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): PZ0217
CAS号: 1373615-35-0
MDL号: MFCD24387542
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$354.21

说明

生化/生理作用

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.
 
PF-5274857 是一种刺猬 (Hh) 信号通路抑制剂,作为一种有效的选择性平滑 (Smo) 拮抗剂,IC50 为 5.8 nM,Ki 为 4.6 nM。 PF-5274857 完全阻断了 Gli-Luc 小鼠胚胎成纤维细胞 (MEF) 中下游基因 Gli1 的转录活性,IC50 为 2.7 nM。 PF-5274857 是脑渗透剂。 化合物 PF-5274857 在小鼠成神经管细胞瘤模型中显示出抗肿瘤活性,体内 IC50 为 8.9 nM。
 

其他说明

This compound was developed by Pfizer for Cytokines & Growth Factors research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
 

法律信息

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

mfr. no.

Pfizer®

颜色

white to beige

溶解性

H2O: 3 mg/mL, clear (warmed)

创始人

Pfizer

储存温度

room temp

SMILES string

O=C(CCS(C)(=O)=O)N(CC1)CCN1C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2.Cl

InChI

1S/C20H25ClN4O3S.ClH/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;1H

InChI key

GULNFUQAVPTTQV-UHFFFAOYSA-N

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.常温阴凉避光
全球实时库存 Availability √美国St. Louis ≥ 99 | 欧洲Eur. ≥ 10 | 東京Tokyo ≥ 22 | 香港与北京 ≥ 32