CYC116|5mg|K1376-上海高创化学科技有限公司

SKU:K1376		M. Wt:368.46
Formula:C18H20N6OS		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:693228-63-6, 1067881-58-6		Synonyms:N/A
Chemical NameN/A

Description	CYC116
Targets	Aurora kinase A	Aurora kinase B
IC50	8 nM(Ki)	9 nM(Ki)
In vitro	CYC116, the most aurora-selective aurora kinase inhibitors, can inhibit aurora A and B kinases about 50-fold more potently than any of the CDKs assayed. CYC116 inhibits two tyrosine kinases, FMS-like tyrosine kinase 3 (FLT3) and vascular endothelial growth factor receptor 2 kinase (VEGFR2), with a Ki value of 44 nM. CYC116 shows no inhibition to PKA, Akt/PKB, PKC, GSK-3alpha, GSK-3beta, ERK2, CaMKII, CK2, Plk1 and SAPK2A. CYC116 shows low micromolar activity against 70 kDa ribosomal protein S6 kinase (p70S6K), Src, and lymphocyte-specific protein tyrosine kinase (Lck). CYC116 is particularly cytotoxic against the acute myelogenous leukemia cell line MV4-11. Treatment with 1.25 uM CYC116 for 7 h results in complete inhibition of histone H3 phosphorylation. CYC116 inhibits autophosphorylation of both aurora A and B(66) at antiproliferative concentrations in cells. [1]
In vivo	In the P388/D1 murine leukemia model, oral dosing at 45 and 67 mg/kg twice daily on days 1?5 and 7?9 resulted in a significant increase in lifespan (ILS) of 172% and 183%, respectively. In NCI-H460 xenografts, at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. [1]
Clinical Trials	N/A
Features	N/A

Description

CYC116

Targets

Aurora kinase A

Aurora kinase B

IC50

8 nM(Ki)

9 nM(Ki)

In vitro

CYC116, the most aurora-selective aurora kinase inhibitors, can inhibit aurora A and B kinases about 50-fold more potently than any of the CDKs assayed. CYC116 inhibits two tyrosine kinases, FMS-like tyrosine kinase 3 (FLT3) and vascular endothelial growth factor receptor 2 kinase (VEGFR2), with a Ki value of 44 nM. CYC116 shows no inhibition to PKA, Akt/PKB, PKC, GSK-3alpha, GSK-3beta, ERK2, CaMKII, CK2, Plk1 and SAPK2A. CYC116 shows low micromolar activity against 70 kDa ribosomal protein S6 kinase (p70S6K), Src, and lymphocyte-specific protein tyrosine kinase (Lck). CYC116 is particularly cytotoxic against the acute myelogenous leukemia cell line MV4-11. Treatment with 1.25 uM CYC116 for 7 h results in complete inhibition of histone H3 phosphorylation. CYC116 inhibits autophosphorylation of both aurora A and B(66) at antiproliferative concentrations in cells. [1]

In vivo

In the P388/D1 murine leukemia model, oral dosing at 45 and 67 mg/kg twice daily on days 1?5 and 7?9 resulted in a significant increase in lifespan (ILS) of 172% and 183%, respectively. In NCI-H460 xenografts, at dose levels of 75 and 100 mg/kg q.d. causes tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively. [1]

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】

CYC116由上海高创化学科技有限公司为您提供，货号K1376，规格：5mg，CAS号：693228-63-6，如您想了解更多关于CYC116价格、CYC116结构式、批发、用途等信息，欢迎咨询。除供应CYC116外，还可为您提供特级新生牛血清（无噬菌体低内毒素）、重组人半乳糖凝集素8/Human LGALS8 His、超级新生牛血清（无支原体）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。