Formulation: A crystalline solid
Formal Name: 3-methyl-N-[1,4,5,6-tetrahydro-6,6-dimethyl-5-[(1-methyl-4-piperidinyl)carbonyl]pyrrolo[3,4-c]pyrazol-3-yl]-butanamide
Purity: ≥95%
Formula Markup: C19H31N5O2
Formula Weight: 361,5
Shelf life (days): 1460
CAS Number: 718630-59-2
Notes: PHA-793887 is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 8, 8, 5, and 10 nM for Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H, respectively).{30703} It is selective for these CDKs over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T1, and glycogen synthase kinase 3β (GSK3β; IC50s = 60, 62, 138, and 79 nM, respectively), as well as a panel of 36 other kinases at 10 µM. PHA-793887 inhibits the proliferation of A2780 ovarian, HCT116 colon, and BxPC-3 pancreatic cancer cells (IC50s = 88, 163, and 3,444 nM, respectively). It inhibits reactivation of latent HIV-1 induced by prostratin (Item No. 10272), panobinostat (Item No. 13280), or JQ-1 in 24ST1NLESG cells (IC50s = 0.004, 0.0082, and 0.016 µM, respectively).{54093} PHA-793887 (20 mg/kg) reduces tumor growth and increases survival in HL-60 and K562 leukemia mouse xenograft models.{30704}
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