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HY-10012

CAS:602306-29-6

602306-29-6  Technical Data: Price and Availability of  Cas No:602306-29-6

Cas : 602306-29-6 M.Wt: 371.4566
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
USD
10mg/$60 In-stock
50mg/$180 In-stock
100mg/$320 In-stock
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602306-29-6  Data Sheet:
 
Introduction of 602306-29-6 :
AZD-5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It also inhibits GSK3β, but is less potent to CDK5/6. IC50 & Target: IC50: 16 nM (CDK1), 6 nM (CDK2), 20 nM (CDK9) [1] In Vitro: AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC50, 6, 45, 16, 21, and 20 nM, respectively). AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC50, 6, 45, 16, 21, and 20 nM, respectively). In common with many other cdk inhibitors, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β in vitro (IC50, 14 and 17 nM, respectively)[1]. AZD5438 significantly augments cellular radiosensitivity in NSCLC cells. Combined treatment with AZD5438 and irradiation also enhances tumor growth delay, with an enhancement factor ranging from 1.2-1.7[2]. In Vivo: AZD5438 (50 mg/kg twice daily or 75 mg/kg, p.o.) inhibits human tumor xenograft growth. In vivo, AZD5438 reduces the proportion of actively cycling cells. Further pharmacodynamic analysis of AZD5438-treated SW620 xenografts shows that efficacious doses of AZD5438 (>40% tumor growth inhibition) maintains suppression of biomarkers, such as phospho-pRbSer249/Thr252, for up to 16 hours following a single oral dose[1].
 
References on 602306-29-6 :
 

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