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AZD-5438

Chemical Structure : AZD-5438

CAS No.: 602306-29-6

AZD-5438 (AZD 5438;AZD5438)

Catalog No.: PC-42060Not For Human Use, Lab Use Only.

AZD-5438 (AZD5438) potent and oral inhibitor of CDK1/2/9 with IC50 of 16/6/20 nM, respectively.

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1 mg (Free Sample) $18 In stock
5 mg $78 In stock
10 mg $118 In stock
50 mg $328 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AZD-5438 (AZD5438) potent and oral inhibitor of CDK1/2/9 with IC50 of 16/6/20 nM, respectively.
AZD-5438 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.
AZD-5438 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.
AZD-5438 inhibits the human tumor xenograft growth in vivo.
AZD-5438 also inhibits PASTA kinase in L. monocytogenes (PrkA) and L. monocytogenes growth in a β-lactam-synergism-dependent manner.

Physicochemical Properties

M.Wt 371.4566
Formula C18H21N5O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Pyrimidinamine, 4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-

References

1. Byth KF, et al. Mol Cancer Ther. 2009 Jul;8(7):1856-66.

2. Boss DS, et al. Ann Oncol. 2010 Apr;21(4):884-94.

3. Pensinger DA, et al. Antimicrob Agents Chemother. 2014 Aug;58(8):4486-94.

4. Raghavan P, et al. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e507-14.

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