AT-7519Hydrochloride , 10mMinDMSO , 902135-91-5

CAS NO.：902135-91-5

Empirical Formula: C16H18Cl3N5O2

Molecular Weight: 418.7

MDL number: MFCD14636428

PRODUCT Properties

• storage temp.: Store at -20°C
• solubility: ≥29.93 mg/mL in H2O; ≥43.3 mg/mL in DMSO with ultrasonic; ≥8.82 mg/mL in EtOH with ultrasonic
• form: crystalline solid
• color: White to off-white
• InChI: InChI=1S/C16H17Cl2N5O2.ClH/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);1H
• InChIKey: PAOFPNGYBWGKCO-UHFFFAOYSA-N
• SMILES: N(C1=CNN=C1C(=O)NC1CCNCC1)C(C1C(=CC=CC=1Cl)Cl)=O.Cl

Description and Uses

AT7519 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) with IC₅₀ values of 210, 47, 100, 13, 170, and <10 nM for Cdk1, 2, 4, 5, 6, and 9, respectively. It is less potent against Cdk3 and Cdk7 and inactive against non-Cdk kinases save for GSK3β (IC₅₀ = 89 nM). AT7519 demonstrates antiproliferative activity against a wide variety of human tumor cell lines (IC₅₀s = 40-940 nM in vitro), inhibiting cell cycle progression and inducing apoptosis, and prevents tumor growth in human tumor xenograft models. AT7519 induces activation of GSK3β by down-regulating GSK3β phosphorylation, which contributes to AT7519-induced apoptosis.

4-(2,6-DichlorobenzoylaMino)-1H-pyrazole-3-carboxylic Acid Piperidin-4-ylaMide Monohydrochloride is used in the structure based design of a cyclin-dependant kinase CDK2 inhibitor.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501