Palbociclib D8 (PD 0332991 D8) 是一种氘标记的 Palbociclib。 Palbociclib 是一种选择性和口服活性的 CDK4 和 CDK6 抑制剂，IC50 分别为 11 和 16 nM。 Palbociclib 具有用于 ER 阳性和 HER2 阴性乳腺癌研究的潜力。
| Cas No. | 1628752-83-9 |
| 别名 | 帕博西尼-D8,PD 0332991-d8 |
| Canonical SMILES | O=C1N(C2CCCC2)C3=NC(NC4=NC=C(N5C([2H])([2H])C([2H])([2H])NC([2H])([2H])C5([2H])[2H])C=C4)=NC=C3C(C)=C1C(C)=O |
| 分子式 | C24H21D8N7O2 |
| 分子量 | 455.6 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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