舒尼替尼 D10 (SU 11248 D10) 是一种氘标记的舒尼替尼。舒尼替尼是一种多靶点受体酪氨酸激酶抑制剂，对 VEGFR2 和 PDGFRβ 的 IC50 分别为 80 nM 和 2 nM。 Sunitinib 是一种 ATP 竞争性抑制剂，通过抑制自身磷酸化和随后的 RNase 激活，有效抑制 Ire1α 的自身磷酸化。
货号:ajcx23542
CAS:1126721-82-1
分子式:C22H17D10FN4O2
分子量：408.5
溶解度:DMSO: Soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Sunitinib-d₁₀is 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 (K_i= 9 nM), PDGFRβ (K_i= 8 nM), and FLT3.^1,2It 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.²Sunitinib 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).^1,2It 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.²Formulations 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)