Sunitinib-d10 |
رقم الكتالوجGC48118 |
Sunitinib D10 (SU 11248 D10) هو الديوتيريوم المسمى SunitinibSunitinib هو مثبط لمستقبلات التيروزين كيناز متعدد الأهداف مع IC50s من 80 نانومتر و 2 نانومتر لـ VEGFR2 و PDGFRβ ، على التواليSunitinib ، مثبط تنافسي لـ ATP ، يمنع بشكل فعال الفسفرة الذاتية لـ Ire1α عن طريق تثبيط الفسفرة الذاتية وتفعيل RNase الناتج
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1126721-82-1
Sample solution is provided at 25 µL, 10mM.
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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