Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl-2,2,3,3,5,5,6,6-d8)-2-pyridinyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one
Purity: ≥99% deuterated forms (d1-d8)
Formula Markup: C24H21D8N7O2
Formula Weight: 455.58152
CAS Number: 1628752-83-9
Notes: PD 0332991-d8 is intended for use as an internal standard for the quantification of PD 0332991 (Item No. 16273) by GC- or LC-MS. PD 0332991 is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases.{28137} It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest at nanomolar concentrations. PD 0332991 can inhibit the growth of certain ER-positive or HER2-amplified breast cancer cells (IC50s as low as 4 nM) and demonstrates synergy with tamoxifen (Item No. 13258) and trastuzumab, respectively.{28138} PD 0332991 inhibition of Cdk4 activity has been used to demonstrate a role for insulin-activated cyclin D1-Cdk4 signaling in the control of glucose metabolism that is independent of cell cycle progression.{26552}
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