SML1855

AZD5438

≥97% (HPLC)

• Synonym(e): 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine, AZD 5438, AZD-5438
• Empirische Formel (Hill-System): C₁₈H₂₁N₅O₂S
• CAS-Nummer: 602306-29-6
• Molekulargewicht: 371.46
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• 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

Beschreibung

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.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable