Description
AT7519 can inhibit CDK1, CDK2, CDK4, CDK5, and CDK6 with IC50 of 210 nM, 14 nM, 100 nM, 13 nM and 170 nM.
Storage
2 years at -20centigrade Powder
Targets
CDK1, CDK2, CDK4, CDK5, CDK6
Molecular Formula
C16H17Cl2N5O2
Chemical Name
4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide
Solubility
DMSO 10 mg/mL Water
In vitro
By binding within the active site cleft of the enzyme overlapping with the ATP-binding site, AT7519 can CDK1, CDK2, CDK4 to CDK6, and CDK9 with IC 50 values of 210, 47, 100, 13, 170, and <10 nmol/L, respectively. The inhibition of CDK1 by AT7519 is competitive with ATP, with a Ki value of 38 nmol/L. AT7519 can also inhibit GSK-3beta with IC50 of 89 nM. AT7519 can inhibit HCT116, A2780 and MRC 5 cell line with IC50 of 82 nM, 350 nM and 980 nM. AT7519 potently inhibited proliferation irrespective of tumor cell source with IC 50 values ranging from 40 to 940 nmol/L for the 26 tumor cell line types.
In vivo
AT7519 inhibited the growth of early-stage HCT116 tumor xenografts at doses of 4.6 and 9.1 mg/kg/dose when given twice in a 24 h period, at 0 h, 8 h later, and 24 h following initial dose for 9 consecutive days
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