CYC116|5mg|K1376-上海高创化学科技有限公司

CYC116

参考价：¥836

供货周期：

一周

品牌：

规格：

5mg

货号：

K1376

CAS号：

693228-63-6

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