|N-(2-((6-(3-(2,6-二氯-3,5-二甲氧苯基)-1-甲基脲基)嘧啶-4-基)氨基)-5-(4-乙基哌嗪-1-基)苯基)丙烯酰胺|CsnPharm

CAS No.: 1702259-66-2

N-(2-((6-(3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide Catalog No. CSN18841

Synonyms: H3 Biomedicine

H3B-6527 acts as a selective FGFR4 inhibitor (IC50 <1.2 nM) over FGFR1-3.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Activation of the fibroblast growth factor receptor FGFR4 by fibroblast growth factor (FGF)19 drives hepatocellular carcinoma (HCC), a disease with few effective treatment options. H3B-6527 is a highly selective and orally available small molecule inhibitor of FGFR4 with an IC₅₀ less than 1.2 nM. In a HCC cell line Hep3B, H3B-6527 (1 nM; 24 h) caused a robust increase in CYP7A1 transcripts suggesting strong inhibition of the FGFR4 pathway by H3B-6527. Further, the levels of pERK1/2 decreased in a dose-dependent manner with maximal inhibition occurring at 100 nM of H3B-6527. In the Hep3B human HCC xenograft mouse model, treatment with H3B-6527 inhibited Hep3B xenograft growth, with the 300 and 100 mg/kg twice-daily doses significantly inhibiting growth and inducing CR (complete regression) or PR (partial regression) in 8 of 8 and 6 of 8 of mice, respectively (TGI (tumor growth inhibition) of 115 and 109%, P<0.05, for the 300 and 100 mg/kg treatment groups, respectively). H3B-6527 is currently undergoing evaluation in a phase I clinical trial in HCC^[3].
作用机制H3B-6527 has an acrylamide group that forms a covalent bond via Michael addition with the Cys552 on FGFR4, present in the hinge region of the ATP-binding pocket^[2].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02834780	Advanced Hepatocellular Carcin... more >>oma Intrahepatic Cholangiocarcinoma Hepatocellular Carcinoma Liver Cancer Liver Neoplasms Hepatic Cancer Hepatic Carcinoma Cholangiocarcinoma Bile Duct Cancer Collapse <<	Phase 1	Recruiting	June 2020	-
NCT03424577	Healthy Participants	Phase 1	Completed	-	United States, Texas ... more >> Worldwide Clinical Trials San Antonio, Texas, United States, 78217 Collapse <<

参考文献

[1] US9730931
[2] Rioux N, Kim A, Nix D, Bowser T, Warmuth M, Smith PG, Schindler J. Effect of a high-fat meal on the relative bioavailability of H3B-6527, a novel FGFR4 inhibitor, in healthy volunteers. Cancer Chemother Pharmacol. 2019 Jan;83(1):91-96
[3] Joshi JJ, Coffey H, Corcoran E. et al. H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma. Cancer Res. 2017 Dec 15;77(24):6999-7013

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5885 mL
- 7.9423 mL
- 15.8847 mL
- 5 mM
- 0.3177 mL
- 1.5885 mL
- 3.1769 mL
- 10 mM
- 0.1588 mL
- 0.7942 mL
- 1.5885 mL

技术信息

CAS号

1702259-66-2

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H34Cl2N8O4

运输

蓝冰

分子量

629.54

别名

H3 Biomedicine

溶解度

DMSO	50.0 mg/mL (79.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

N-(2-((6-(3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide Catalog No. CSN18841

靶点选择性

请登录您的专属账户

确认信息