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  • Sunitinib-d10
Sunitinib-d10的可视化放大

Sunitinib-d10

An internal standard for the quantification of sunitinib

原价
¥7662-7662
价格
6130-6130
Sunitinib-d10的二维码

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  • 货号: ajcx23542
  • CAS: 1126721-82-1
  • 别名: 舒尼替尼-D10,SU 11248-d10
  • 分子式: C22H17D10FN4O2
  • 分子量: 408.5
  • 纯度: >98%
  • 溶解度: DMSO: Soluble
  • 储存: Store at -20°C
  • 库存: 现货

Background

Sunitinib-d10 is intended for use as an internal standard for the quantification of sunitinib by GC- or LC-MS. Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFRβ (Ki = 8 nM), and FLT3.1,2 It is at least 10-fold selective for FLK1 and PDGFRβ over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl, and Src.2 Sunitinib inhibits VEGF-dependent FLK1 and PDGF-dependent PDGFRβ phosphorylation (IC50s = 10 and 10 nM, respectively) as well as phosphorylation of FLT3 and FLT3 carrying the activating internal tandem duplication mutation (FLT3-ITD; IC50s = 250 and 50 nM, respectively).1,2 It decreases VEGF- and FGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50s = 30 and 700 nM, respectively) and reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 20 to 80 mg/kg per day.2 Formulations containing sunitinib have been used in the treatment of gastrointestinal stromal tumors and metastatic renal cell carcinoma.



1.O'Farrell, A.M., Abrams, T.J., Yuen, H.A., et al.SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivoBlood101(9)3597-3605(2003) 2.Mendel, D.B., Laird, A.D., Xin, X., et al.In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: Determination of a pharmacokinetic/pharmacodynamic relationshipClin. Cancer Res.9(1)327-337(2003)

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