Pazopanib-d6 (GW786034-d6) 是氘标记的 Pazopanib。 Pazopanib (GW786034) 是一种新型多靶点 VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1 和 c-Fms 抑制剂，IC50 分别为 10、30、47、84、74、140 和 146 nM。
| Cas No. | 1219592-01-4 |
| 别名 | 培唑帕尼-d6,GW786034-d6 |
| Canonical SMILES | CC(C(S(N)(=O)=O)=C1)=CC=C1NC2=NC=CC(N(C([2H])([2H])[2H])C3=CC4=NN(C([2H])([2H])[2H])C(C)=C4C=C3)=N2 |
| 分子式 | C21H17D6N7O2S |
| 分子量 | 443.6 |
| 溶解度 | DMF: 16 mg/ml,DMSO: 16 mg/ml |
| 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 | Pazopanib-d6 is intended for use as an internal standard for the quantification of pazopanib by GC- or LC-MS. Pazopanib is a multi-kinase inhibitor that inhibits the VEGF receptors VEGFR1, VEGFR2, and VEGFR3 (IC50s = 10, 30, and 47 nM, respectively, in a cell-free enzyme assay). It also inhibits PDGFRα, PDGFRβ, and c-Kit (IC50s = 71, 84, and 74 nM, respectively, in a cell-free enzyme assay) as well as additional receptor tyrosine kinases. Pazopanib inhibits upregulation of the surface adhesion proteins ICAM-1 and VCAM-1 induced by VEGF in multiple myeloma cells cocultured with human umbilical vein endothelial cells (HUVECs) and decreases multiple myeloma cell adhesion to HUVECs. It also inhibits proliferation of multiple myeloma cells cocultured with HUVECs. Pazopanib (30 and 100 mg/kg) reduces tumor growth, induces apoptosis, decreases angiogenesis, and increases survival in a multiple myeloma mouse xenograft model. Formulations containing pazopanib have been used in the treatment of cancer. |
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