A CDK inhibitor
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PHA-793887

Item No. 18388

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
718630-59-2
Molecular Formula
C19H31N5O2
Formula Weight
361.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
235 nm
SMILES
CN1CCC(C(N2C(C)(C)C(NN=C3NC(CC(C)C)=O)=C3C2)=O)CC1
InChi Code
InChI=1S/C19H31N5O2/c1-12(2)10-15(25)20-17-14-11-24(19(3,4)16(14)21-22-17)18(26)13-6-8-23(5)9-7-13/h12-13H,6-11H2,1-5H3,(H2,20,21,22,25)
InChi Key
HUXYBQXJVXOMKX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    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).1 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).2 PHA-793887 (20 mg/kg) reduces tumor growth and increases survival in HL-60 and K562 leukemia mouse xenograft models.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brasca, M.G., Albanese, C., Alzani, R., et al. Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioor. Med. Chem. 18(5), 1844-1853 (2010).

    2. Vargas, B., Giacobbi, N.S., Sanyal, A., et al. Inhibitors of signaling pathways that block reversal of HIV-1 latency. Antimicrob. Agents Chemother. 63(2), e01744-01718 (2019).

    3. Alzani, R., Pedrini, O., Albanese, C., et al. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Exp. Hematol. 38, 259-269 (2010).