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苏尼替尼

规格或纯度: 99%
有货

库存信息

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库存信息

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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
S126061-250mg
250mg 现货 Stock Image
S126061-1g
1g 现货 Stock Image
S126061-5g
5g 现货 Stock Image
S126061-25g
25g 现货 Stock Image

基本描述

别名 舒尼替尼
英文别名 1H-Pyrrole-3-carboxamide,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-|D08552|C22H27FN4O2|N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1 pound not2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2 pound not4-dimethyl-1H-pyrrole-3-carboxamide|SCHEMBL510
规格或纯度 99%
英文名称 Sunitinib
生化机理 IC50 Value: 2 nM (PDGFRβ); 80 nM (VEGFR2) [1] Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. in vitro: Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively [2]. SU11248 also has potent activity against wild-type FLT3 (FLT3-WT), FLT3-ITD, and FLT3 activation loop (FLT3-Asp835) mutants in phosphorylation as
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 100mg卖完停产,不再备货
产品介绍

Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

名称和标识符

PubChem SID 488195369
IUPAC Name N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
INCHI InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChi Key WINHZLLDWRZWRT-ATVHPVEESA-N
Canonical SMILES CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C
Isomeric SMILES CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C
PubChem CID 5329102
UN Number 2811
Packing Group III
分子量 398.47

化学和物理性质

溶解性 25°C: DMSO

安全和危险性(GHS)

象形图
ghs06

Toxic

信号词 Danger
危险声明 H372: Causes damage to organs through prolonged or repeated exposure
H360: May damage fertility or the unborn child
预防措施声明 P280,P405,P501,P264,P260,P201,P308+P313,P270,P202

质检证书(COA)

质检报告(COA)

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参考文献

1. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB et al..  (2003)  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 relationship..  Clin Cancer Res,  (1):  (327-37).  [PMID:12538485]
2. Khanwelkar RR, Chen GS, Wang HC, Yu CW, Huang CH, Lee O, Chen CH, Hwang CS, Ko CH, Chou NT et al..  (2010)  Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors..  Bioorg Med Chem,  18  (13):  (4674-86).  [PMID:20570526]