CAS NO: | 1628752-83-9 |
规格: | 98% |
分子量: | 455.6 |
包装 | 价格(元) |
500ug | 电议 |
1mg | 电议 |
Background:
PD 0332991-d8 is intended for use as an internal standard for the quantification of PD 0332991 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. 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 and trastuzumab, respectively. 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.