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 (Synonyms  AZD 5438;AZD5438)
602306-29-6  Technical Data: Price and Availability of  Cas No:602306-29-6

Cas : 602306-29-6 M.Wt: 371.46
Cas : 602306-29-6 Formula: C18H21N5O2S
Cas : 602306-29-6 Purity: >98 %
Cas : 602306-29-6 Storage: at 20℃ 2 years
Cas : 602306-29-6 Solubility: 10 mM in DMSO
Cas : 602306-29-6 Name: AZD-5438
10mg/$60 In-stock
50mg/$220 In-stock
100mg/$395 In-stock
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>10g Get quote
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602306-29-6  Data Sheet:
Introduction of 602306-29-6 :
AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6. IC50 Value: 16 nM(CDK1); 6 nM(CDK2); 20 nM(CDK9) Target: CDK in vitro: AZD5438 exhibits the potent inhibitory effect on activity of cyclin-dependent kinases including cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, cyclin D3-cdk6, and cyclin T-cdk9 with IC50 of 6 nM, 45 nM, 16 nM, 21 nM, and 20 nM, respectively. Besides, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β with IC50 of 14 nM and 17 nM, respectively. AZD5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates, and exhibits the broad antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50 ranging from 0.2 μM (MCF-7) to 1.7 μM (ARH-77). in vivo: AZD-5438 blocks cell cycling at G2-M, S and G1 phases; reduces the proportion of actively cycling cells in vivo. oral treatment of AZD5438 leads to statistically significant inhibition against the growth of human tumor xenografts derived from a wide range of different cancer types including breast, colon, lung, prostate, and ovarian with maximum TGI ranging from 38% to 153%. In the SW620 xenograft model, AZD5438 causes the inhibition of several cell cycle proteins such as, phH3, phosphonucleolin, PP1a, and several phospho-pRb epitopes in a dose-dependent manner.
References on 602306-29-6 :

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