PD 0332991-d8 (Synonyms: Palbociclib-d8) |
Catalog No.GC40092 |
팔보시클립 D8(PD 0332991 D8)은 팔보시클립으로 표지된 중수소입니다. 팔보시클립은 각각 11 및 16 nM의 IC50을 갖는 선택적 및 경구 활성 CDK4 및 CDK6 억제제입니다. 팔보시클립은 ER-양성 및 HER2-음성 유방암 연구에 대한 가능성이 있습니다.
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Cas No.: 1628752-83-9
Sample solution is provided at 25 µL, 10mM.
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.
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