CH5424802|2mg|K1371-上海高创化学科技有限公司

SKU:K1371		M. Wt:482.62
Formula:C30H34N4O2		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:1256580-46-7		Synonyms:N/A
Chemical NameN/A

Description	CH5424802
Targets	ALK
IC50	1.9 nM
In vitro	CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 completely inhibits the phosphorylation of STAT3 at Tyr705. CH5424802 is preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCI-H522 cells (EGFR wild-type, KRAS wild-type, and ALK wild-type) in monolayer culture.
In vivo	The half-life and the oral bioavailability of CH5424802 in mice are 8.6 hours and 70.8%, respectively. At a repeated dose of 6 mg/kg, the mean plasma levels reached 1.7, 1.5, and 0.3 nM at 2, 7, and 24 hours post-dose, respectively. Administration of CH5424802 leads to tumor growth prevention and tumor regression. Tumor growth inhibition at 20 mg/kg is 119% for KARPAS-299 and 104% for NB-1 on day 20. CH5424802 inhibits the phosphorylation of STAT3 in a dose-dependent manner (20 mg/kg).
Clinical Trials	N/A
Features	N/A

Description

CH5424802

Targets

ALK

IC50

1.9 nM

In vitro

CH5424802 prevents autophosphorylation of ALK in NCI-H2228 NSCLC cells expressing EML4-ALK. CH5424802 also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 completely inhibits the phosphorylation of STAT3 at Tyr705. CH5424802 is preferentially efficacious against NCI-H2228 cells expressing EML4-ALK, but not ALK fusion-negative NSCLC cell lines, including HCC827 cells (EGFR exon 19 deletion), A549 cells (KRAS mutant), or NCI-H522 cells (EGFR wild-type, KRAS wild-type, and ALK wild-type) in monolayer culture.

In vivo

The half-life and the oral bioavailability of CH5424802 in mice are 8.6 hours and 70.8%, respectively. At a repeated dose of 6 mg/kg, the mean plasma levels reached 1.7, 1.5, and 0.3 nM at 2, 7, and 24 hours post-dose, respectively. Administration of CH5424802 leads to tumor growth prevention and tumor regression. Tumor growth inhibition at 20 mg/kg is 119% for KARPAS-299 and 104% for NB-1 on day 20. CH5424802 inhibits the phosphorylation of STAT3 in a dose-dependent manner (20 mg/kg).

Clinical Trials

N/A

Features

N/A

工商信息

企业名称

上海高创化学科技有限公司

企业信息已认证

企业类型

信用代码

310228001353263

成立日期

2010-06-05

注册资本

经营范围

从事化学科技、计算机领域内技术开发、技术咨询、技术服务,从事生物科技领域内技术开发、技术咨询,化学试剂、化工原料及产品(除危险化学品、监控化学品、烟花爆竹、民用爆炸物品、易制毒化学品),实验室设备(除医疗器械),仪器仪表,Ⅰ类医疗器械,金属制品,电子产品,机电产品销售。【依法须经批准的项目,经相关部门批准后方可开展经营活动】

CH5424802由上海高创化学科技有限公司为您提供，货号K1371，规格：2mg，CAS号：1256580-46-7，如您想了解更多关于CH5424802价格、CH5424802结构式、批发、用途等信息，欢迎咨询。除供应CH5424802外，还可为您提供大鼠胆囊收缩素/缩胆囊素八肽(CCK-8)ELISA Kit、重组人半乳糖凝集素16/LGALS16 Human、重组人卵泡抑素/Human FST His等试剂，公司有专业的客户服务团队，是您值得信赖的合作伙伴，上海高创客户服务电话，售前、售后均可联系。