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![2-Chloro-N-[4-chloro-3-(2-pyridinyl)phenyl]-4-(methylsulfonyl)benzamide AldrichCPR](/deepweb/assets/sigmaaldrich/product/structures/378/828/9834c930-f37e-4730-8e9c-00a587e5421d/640/9834c930-f37e-4730-8e9c-00a587e5421d.png)
质量水平
方案
≥97% (HPLC)
表单
powder
颜色
yellow to orange
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
[S](=O)(=O)(C)c1ccc(cc1)Nc2nc(ccn2)c3[n](c(nc3)C)C(C)C
InChI
1S/C18H21N5O2S/c1-12(2)23-13(3)20-11-17(23)16-9-10-19-18(22-16)21-14-5-7-15(8-6-14)26(4,24)25/h5-12H,1-4H3,(H,19,21,22)
InChI key
WJRRGYBTGDJBFX-UHFFFAOYSA-N
生化/生理作用
AZD5438 is an orally active, potent and reversible inhibitor against cyclin-dependent kinases (IC50 = 6 nM/Cyc E-CDK2, 14 nM/p25-CDK5, 16 nM/Cyc B1-CDK1, 20 nM/Cyc T-CDK9, 21 nM/Cyc D3-CDK6, 45 nM/Cyc A-CDK2, 449 nM/Cyc D1-CDK4, 821 nM/Cyc H-CDK7; [ATP] = Km) and glycogen synthase kinase GSK-3β≤ (IC50 = 17 nM) without significant inhibitory potency toward 30 other kinases (≤75% inhibition at 10 μM). AZD5438 effectively inhibits cellular CDK substrates phosphorylation and displays antiproliferation activity against a broad spectrum of human cancer cultures (IC50 from 0.2 μM/MCF to 1.7 μM/ARH-77) by inducing cell cycle arrest at G2-M, S, and G1. Oral administration (50 mg/kg/12 h or 75 mg/kg/day) is efficacious against human tumor xenograft growth in mice in vivo.
AZD5438 is an orally active, potent and reversible inhibitor against cyclin-dependent kinases.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
Camille D A Terfve et al.
Nature communications, 6, 8033-8033 (2015-09-12)
Mass spectrometry is widely used to probe the proteome and its modifications in an untargeted manner, with unrivalled coverage. Applied to phosphoproteomics, it has tremendous potential to interrogate phospho-signalling and its therapeutic implications. However, this task is complicated by issues
Kate F Byth et al.
Molecular cancer therapeutics, 8(7), 1856-1866 (2009-06-11)
Deregulation of the cell cycle has long been recognized as an essential driver of tumorigenesis, and agents that selectively target key cell cycle components continue to hold promise as potential therapeutics. We have developed AZD5438, a 4-(1-isopropyl-2-methylimidazol-5-yl)-2-(4-methylsulphonylanilino) pyrimidine, as a
Nozomi Tomimatsu et al.
Nature communications, 5, 3561-3561 (2014-04-08)
Resection of DNA double-strand breaks (DSBs) is a pivotal step during which the choice between NHEJ and HR DNA repair pathways is made. Although CDKs are known to control initiation of resection, their role in regulating long-range resection remains elusive.
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