AZD5438
SIGMA/SML1855 - ≥97% (HPLC)
Synonym: 4-
CAS Number: 602306-29-6
Empirical Formula (Hill Notation): C18H21N5O2S
Molecular Weight: 371.46
Linear Formula: C18H21N5O2S
Product Type: Chemical
| assay | ≥97% (HPLC) |
| color | yellow to orange |
| form | powder |
| Quality Level | 100  |
| solubility | DMSO: 20 mg/mL, clear |
| storage temp. | 2-8°C |
| 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 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥97% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |