PD 0332991-d8 (Synonyms: Palbociclib-d8) |
| カタログ番号GC40092 |
パルボシクリブ D8 (PD 0332991 D8) は、パルボシクリブと標識された重水素です。パルボシクリブは、選択的かつ経口的に活性な CDK4 および CDK6 阻害剤であり、IC50 はそれぞれ 11 および 16 nM です。 Palbociclib は、ER 陽性および HER2 陰性の乳がん研究の可能性を秘めています。
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Cas No.: 1628752-83-9
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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