AZD5438

AZD5438

Stock Code: 3575462
Manufacturer Part No: SML1855-25MG
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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.


Packaging


5, 25 mg in glass bottle

Colouryellow to orange
Quality Level100
ManufacturerSIGMA-ALDRICH
Storage Temp.2-8°C
SolubilityDMSO: 20 mg/mL, clear
Formpowder
Assay≥97% (HPLC)

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