Urea,N-(3-chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]- (1057249-41-8)

 N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea , with the CAS registry number 1057249-41-8, is also named as SNS-314 . It is soluble in DMSO and storage at -20 °C in 2 years.

 N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea is an inhibitor which is ATP-competitive, potent and selective with Aurora kinases A (IC50=9.0nM), B (IC50=31nM), and C (IC50=3.4nM). When screened at 1uM, it demonstrated remarkable specialcity and was found to inhibit only 24 of 219 kinases by greater than 65%. Histone H3 phosphorylation was potently inhibited by N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea in all 6 cell lines tested with IC50 values ranging from 9 nM in HCT116 cellsto 60 nM in Calu-6 cells. N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea also displayed signi?cant anti-tumor activity in mouse xenograft models of human breast (MDA-MB-231), prostate (PC-3), lung (H1299 and Calu-6), ovarian (A2780) carcinomas and melanoma (A375). It represents a new class of highly potent Aurora kinase inhibitors and is being evaluated in a phase-1 dose escalation study designed to assess safety and tolerability in patients with advanced solid malignancies.

The N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea has many suppliers, such as American Custom Chemicals Corp. and Selleck Chemicals LLC in USA.