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Dovitinib-d8
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Dovitinib-d8图片
CAS NO:1246819-84-0
包装:1mg
市场价:4067元

产品介绍
Dovitinib-D8 (CHIR-258-D8) 是氘标记的 Dovitinib。 Dovitinib (CHIR-258) 是一种多靶点酪氨酸激酶抑制剂,对 FLT3、c-Kit、FGFR1/FGFR3、VEGFR1/VEGFR2/ 的 IC50 为 1、2、8/9、10/13/8、27/210 nM VEGFR3 和 PDGFRα/PDGFRβ,分别。
Cas No.1246819-84-0
别名多韦替尼 D8
Canonical SMILESFC1=C2C(NC(C(C3=NC4=C(C=C(N5C([2H])([2H])C([2H])([2H])N(C)C([2H])([2H])C5([2H])[2H])C=C4)N3)=C2N)=O)=CC=C1
分子式C21H13D8FN6O
分子量400.5
溶解度Acetonitrile:Methanol (1:1): soluble,DMSO: soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Dovitinib-d8 is intended for use as an internal standard for the quantification of dovitinib by GC- or LC-MS. Dovitinib is a receptor tyrosine kinase inhibitor that targets vascular endothelial growth factor-2, basic fibroblast growth factor-1, and platelet-derived growth factor β receptors (IC50s = 65, 11, and 5 nM, respectively).1 By impairing these kinase signals, 1 μM dovitinib has been shown to prevent the growth and motility of pancreatic cancer cell lines (HPAF-II, BxPC-3, MiaPaCa2, and L3.6pl).2 At 0.04 μM, dovitinib can inhibit endothelial cell proliferation and motility.3 These antiangiogenic effects have been proposed to be the mechanism by which dovitinib inhibits hepatocellular carcinoma growth and metastasis.3 Dovitinib has been evaluated in clinical trials for the treatment of advanced solid tumors.4,5

|1. Renhowe, P.A., Pecchi, S., Shafer, C.M., et al. Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: A novel class of receptor tyrosine kinase inhibitors. J. Med. Chem. 52(2), 278-292 (2009).|2. Taeger, J., Moser, C., Hellerbrand, C., et al. Targeting FGFR/PDGFR/VEGFR impairs tumor growth, angiogenesis, and metastasis by effects on tumor cells, endothelial cells, and pericytes in pancreatic cancer. Mol. Cancer Ther. 10(11), 2157-2167 (2011).|3. Chen, Z.Y., Shi, M., Peng, L.X., et al. Dovitinib preferentially targets endothelial cells rather than cancer cells for the inhibition of hepatocellular carcinoma growth and metastasis. J. Transl. Med. 10:245, (2012).|4. Kim, K.B., Chesney, J., Robinson, D., et al. Phase I/II and pharmacodynamic study of dovitinib (TKI258), an inhibitor of fibroblast growth factor receptors and VEGF receptors, in patients with advanced melanoma. Clin. Cancer Res. 17(23), 7451-7461 (2011).|5. Sarker, D., Molife, R., Evans, T.R.J., et al. A phase I pharmacokinetic and pharmacodynamic study of TKI258, an oral, multitargeted receptor tyrosine kinase inhibitor in patients with advanced solid tumors. Clin. Cancer Res. 14(7), 2075-2081 (2008).