产品名称

英文名称：AT7519

同义词

AT7519、844442-38-2、AT-7519、4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide、AT 7519、AT7519 Hydrochloride、4-(2,6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide、Cdki at7519、N-(4-Piperidinyl)-4-(2,6-dichloroben

产品性质

CAS编号：844442-38-2

分子式：C16H17Cl2N5O2

分子量：382.24

PubChem编号：11338033

英文别名：AT7519|844442-38-2|AT-7519|4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide|AT 7519|AT7519 Hydrochloride|4-(2,6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide|Cdki at7519|N-(4-Piperidinyl)-4-(2,6-dichloroben

规格或纯度：≥99%

英文名称：AT7519

生化机理：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.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：AT7519是多种CDK抑制剂，作用于CDK1， 2， 4， 6和9时，IC50为10-210 nM，对CDK3作用效果稍弱，对CDK7几乎没有抑制活性。Phase 2。A novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6.AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. Phase 2.A novel small molecule effective as a pan-Cdk inhibitor for Cdk1, Cdk2, Cdk3, Cdk4, Cdk5 and Cdk6.

ALogP：2.6

IUPAC Name：4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide

INCHI：InChI=1S/C16H17Cl2N5O2/c17-10-2-1-3-11(18)13(10)15(24)22-12-8-20-23-14(12)16(25)21-9-4-6-19-7-5-9/h1-3,8-9,19H,4-7H2,(H,20,23)(H,21,25)(H,22,24)

InChi Key：OVPNQJVDAFNBDN-UHFFFAOYSA-N

Canonical SMILES：C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl

Isomeric SMILES：C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl

PubChem CID：11338033

CAS Registry No.：844442-38-2

DiscoveRx TREEspot：AT-7519|

ChEMBL Ligand：CHEMBL445813

RCSB PDB Ligand：LZE

溶解性：Soluble in DMSO (10 mg/ml) at 25°C, water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25°C.

产品包装