PD 0332991 isethionate

• Supplier: Tocris Bioscience
• Catalog: 4192
• Prices: $225.00, $925.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 827022-33-3
• Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-oneisethionatesalt
• Formula: C24H29N7O2.C2H6O4S
• Molecular Weight: 573.66
• Purity: >98 %
• Description: Potent Cdk4/6 inhibitor (IC 50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC 50 values are > 10 μ M). Induces G 1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant.

Product References

Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated - Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated

Fry DW, Harvey PJ, Keller PR, Elliott WL, Meade M, Trachet E, Albassam M, Zheng X, Leopold WR, Pryer NK, Toogood PL. Mol Cancer Ther. 2004 Nov;3(11):1427-38.

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. - Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.

Toogood PL, Harvey PJ, Repine JT, Sheehan DJ, VanderWel SN, Zhou H, Keller PR, McNamara DJ, Sherry D, Zhu T, Brodfuehrer J, Choi C, Barvian MR, Fry DW. J Med Chem. 2005 Apr 7;48(7):2388-406.

Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth - Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth

Michaud K, Solomon DA, Oermann E, Kim JS, Zhong WZ, Prados MD, Ozawa T, James CD, Waldman T. Cancer Res. 2010 Apr 15;70(8):3228-38.