An inhibitor of Cdks
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PHA-848125

Item No. 21474

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
CAS Number
802539-81-7
Synonyms
  • Milciclib
Molecular Formula
C25H32N8O
Formula Weight
460.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
295 nm
SMILES
[H]N(C1=NC(C(N(C)N=C2C(N(C)[H])=O)=C2C(C)(C)C3)=C3C=N1)C(C=C4)=CC=C4N5CCN(C)CC5
InChi Code
InChI=1S/C25H32N8O/c1-25(2)14-16-15-27-24(29-20(16)22-19(25)21(23(34)26-3)30-32(22)5)28-17-6-8-18(9-7-17)33-12-10-31(4)11-13-33/h6-9,15H,10-14H2,1-5H3,(H,26,34)(H,27,28,29)
InChi Key
RXZMYLDMFYNEIM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM).1 It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7.1 PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brasca, M.G., Amboldi, N., Ballinari, D., et al. Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J. Med. Chem. 52(16), 5152-5163 (2009).

    2. Caporali, S., Alvino, E., Starace, G., et al. The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound. Pharmacol. Res. 61(5), 437-448 (2010).

    3. Degrassi, A., Russo, M., Nanni, C., et al. Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-RasG12DLA2 lung adenocarcinoma transgenic mouse model: Evaluation by multimodality imaging. Mol. Cancer Ther. 9(3), 673-681 (2010).