AZD5438 Inhibitor CAS No. 602306-29-6

Cat. No.	Name	Size	Price
KI0104	AZD5438	10 mg	$220
	AZD5438	50 mg	$742.5
	AZD5438	200 mg	$1200

Chemical Characteristic

Product Name	AZD5438
CAS No.	602306-29-6
Molecular Weight	371.46
Formula	C₁₈H₂₁N₅O₂S
Chemical Name	4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
Smiles	c1(nc(ccn1)c1cnc(n1C(C)C)C)Nc1ccc(cc1)S(=O)(=O)C
Chemical Structure

Biological activities

AZD5438 is a potent oral inhibitor of cyclin-dependent kinase (CDK) 1, CDK 2, and CDK 9. The IC50 of AZD5438 is 16, 6, and 20 nM against CDK 1, CDK 2, and CDK 9, respectively. In vitro, AZD5438 reveals significant antiproliferative activity in human tumor cell lines with IC50 ranging from 0.2 µM to 1.7µM, causing inhibition of the phosphorylation of CDK substrates pRb, nucleolin, protein phosphatase 1a, and RNA polymerase II COOH-terminal domain and blocking cell cycling at G(2)-M, S, and G(1) phases.^[1] Treatment of NSCLC cells with AZD5438 significantly augments cellular radiosensitivity. Combined treatment with AZD5438 and irradiation also enhances tumor growth delay.^[2] In vivo, when orally administered at either 50 mg/kg twice daily or 75 mg/kg once daily, AZD5438 suppresses human tumor xenograft growth. In vivo, AZD5438 reduces the proportion of actively cycling cells. AZD5438-treated SW620 xenografts reveal that efficacious doses of AZD5438 (>40% tumor growth inhibition) maintains suppression of biomarkers, such as phospho-pRbSer(249)/Thr(252), for up to 16 hours following a single oral dose.^[1]

Protocols

AZD5438 is prepared in hydroxy-propyl-methyl-cellulose. ^[1]

References

[1] Byth KF, et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009, 8(7): 1856-1866. [2] Raghavan P, er al.AZD5438, an Inhibitor of Cdk1, 2, and 9, Enhances the Radiosensitivity of Non-Small Cell Lung Carcinoma Cells. Int J Radiat Oncol Biol Phys. 2012, 84(4): e507-e514.

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