AG-012986

• Target:

  Others|||CDK

• Related Pathways:

  Others|||Cell Cycle/Checkpoint

• Bioactivity:

  AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC (50) s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser (795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity.

• Smiles:

  C(=O)(C=1SC(NC2=CC=C(C(N[C@@H](CN(C)C)C)=O)C=C2)=NC1N)C3=C(F)C=CC=C3F

• Molecular Formula:

  C22H23F2N5O2S

• Molecular Weight:

  459.51

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  486414-35-1