AZD-5438
A potent and oral inhibitor of CDK1/2/9 with IC50 of 16/6/20 nM, respectively; also inhibits the kinase activity of p25-Cdk5 (IC50=14 nM) and GSK-3β (IC50=17 nM) in vitro, displays 75-fold less active against cyclin D-Cdk4; shows significant antiproliferative activity in human tumor cell lines (IC50 range: 0.2-1.7 uM), inhibits the phosphorylation of Cdk substrates pRb, nucleolin, PP1A, and RNA polymerase II COOH-terminal domain and blocks cell cycle; inhibits the human tumor xenograft growth in vivo; also inhibits PASTA kinase in L. monocytogenes (PrkA) and L. monocytogenes growth in a β-lactam-synergism-dependent manner.Solid Tumors Phase 1 Discontinued.
Product Specifications
CAS Number
602306-29-6
Product Name Alternative
AZD 5438 | AZD5438
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=S (C1=CC=C (NC2=NC=CC (C3=CN=C (C) N3C (C) C) =N2) C=C1) (C) =O
Molecular Formula
C18H21N5O2S
Molecular Weight
371.4566
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Pyrimidinamine, 4-[2-methyl-1- (1-methylethyl) -1H-imidazol-5-yl]-N-[4- (methylsulfonyl) phenyl]-
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POLR3K (DNA-directed RNA Polymerase III Subunit RPC10, RNA Polymerase III Subunit C10, DNA-directed RNA Polymerase III Subunit K, RNA Polymerase III 12.5kD Subunit, RPC12.5, RNA Polymerase III Subunit C11, HsC11p, RPC11, hRPC11, My010, C11-RNP3, RPC12.5)
POLR3K (DNA-directed RNA Polymerase III Subunit RPC10, RNA Polymerase III Subunit C10, DNA-directed RNA Polymerase III Subunit K, RNA Polymerase III 12.5kD Subunit, RPC12.5, RNA Polymerase III Subunit C11, HsC11p, RPC11, hRPC11, My010, C11-RNP3, RPC12.5)