PD 0332991 Isethionate (6-acetyl-8-cyclopentyl-5-methyl-2-[ [5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d] pyrimidin-7(8H)-one isethionate salt)

Potent Cdk4/6 inhibitor (IC50 values are 11 and 15nm for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10um). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant.\n\nSequence:\nC24H29N7O2.C2H6O4S\n\nSolubility:\nDMSO (~10mM), H2O (~100mM) \n\nMolecular Weight:\n~573.66\n\nStorage and Stability:\nMay be stored at 4 degrees C. For long-term storage, aliquot and store at 4 degrees C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.

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SPECIFICATIONS

Catalog Number

145686

Size

10mg

Form

Supplied as a yellow solid.

Purity

~98% (HPLC)

References

1. Fry et al (2004) Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol.Cancer Ther. 3 1427. PMID: 15542782. 2. Toogood et al (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 48 2388. PMID: 15801831. 3. Michaud et al (2010) Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res. 70 3228. PMID: 20354191.