SML1855
AZD5438
≥97% (HPLC)
别名:
4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine, AZD 5438, AZD-5438
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Assay:
≥97% (HPLC)
Form:
powder
Quality Segment
assay
≥97% (HPLC)
form
powder
color
yellow to orange
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
SMILES string
[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
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable