AT7519 CAS: 844442-38-2
MF: C16H17Cl2N5O2
MW: 382.24
A novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6.

AT7519 (CAS 844442-38-2)

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备用名: 4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide
应用; AT7519 is a novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6
CAS号码: 844442-38-2
分子量: 382.24
分子式: C16H17Cl2N5O2
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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AT7519 is a novel small molecule effective as a multi-cyclin-dependent kinase inhibitor for Cdk1/cyclin B (IC50 = 210 nM), Cdk2/Cyclin A (IC50 = 47 nM), Cdk3/Cyclin E (IC50 = 360 nM), Cdk4/Cyclin D1 (IC50 = 100 nM), Cdk5/p35 (IC50 = 13 nM) and Cdk6/Cyclin D3 (IC50 = 170 nM). AT7519 is an ATP competitive Cdk inhibitor with a Ki value of 38 nM for Cdk1. AT7519 is inactive against all non-Cdk kinases with the exception of GSK3β (IC50 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription.

物理状态 :
Solid
溶解度 :
Soluble in DMSO (10 mg/ml) at 25°C, water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25°C.
保存 :
Store at -20° C
熔点 :
285.07° C (Predicted)
沸点 :
~586.0° C at 760 mmHg (Predicted)
密度 :
~1.5 g/cm3 (Predicted)
折射率 :
n20D 1.65 (Predicted)
IC50 :
CDK5/p35: IC50 = 13 nM; CDK2/Cyclin A: IC50 = 47 nM; CDK4/Cyclin D1: IC50 = 100 nM; CDK6/Cyclin D3: IC50 = 170 nM; CDK1/cyclin B: IC50 = 210 nM
Ki 数据 :
CDK1: Ki= 38 nM
pK值 :
pKa: 11.1 (Predicted), pKb: 9.63 (Predicted)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
MDL 号码 :
MFCD13184820
SMILES :
C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl

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PMID: # 25846820  Mol. Neurobiol. 1959-1976.

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