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Sulfatinib

产品编号 T4075 CAS 1308672-74-3

别名: KDR-IN-1, 索凡替尼

Sulfatinib (KDR-IN-1) (HMPL-012) 是一种有效且高度选择性的酪氨酸激酶抑制剂，可抑制VEGFR1/2/3，FGFR1和CSF1R，IC50范围为1 到 24 nM 之间。

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Sulfatinib, CAS 1308672-74-3

规格	价格/CNY	货期
1 mg	￥ 479	现货
5 mg	￥ 1,090	现货
10 mg	￥ 1,730	现货
25 mg	￥ 2,930	现货
50 mg	￥ 4,390	现货
100 mg	￥ 5,970	现货
1 mL * 10 mM (in DMSO)	￥ 795	现货

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纯度: 100%

纯度: 98.93%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.
体外活性	Sulfatinib inhibits VEGFR1, 2, and 3, FGFR1 and CSF1R kinases with IC 50 s in a range of 1 to 24 nM. Sulfatinib strongly blocks VEGF induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1 stimulated CSF1R phosphorylation in RAW264.7 cells with IC 50 of 2 and 79 nM, respectively. Sulfatinib also attenuates VEGF or FGF stimulated HUVEC cells proliferation with IC 50 < 50 nM [1]. Also, it is a hERG inhibitor with IC 50 of 6.8 μM in CHO cell [2].
体内活性	A single oral dosing of Sulfatinib inhibits VEGF stimulated VEGFR2 phosphorylation in lung tissues of nude mice in an exposure-dependent manner in animal studies. Besides, elevation of FGF23 levels in plasma 24 hours post dosing suggests suppression of FGFR signaling. Sulfatinib demonstrates potent tumor growth inhibition in multiple human xenograft models and decreases CD31 expression remarkably, suggesting strong inhibition on angiogenesis through VEGFR and FGFR signaling. In a syngeneic murine colon cancer model CT-26, Sulfatinib demonstrates moderate tumor growth inhibition after single agent treatment [1]. After oral dosing of 10 mg/kg, the AUC and C max are 397 ng/mL and 138ng/mL in the mouse, respectively [1].
激酶实验	The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. Tyr1 peptide is used to test the KDR kinase inhibitory activity of N-(2-(dimethylamino)-ethyl)-1-(3-((4-((2-methyl-1H-indol-5-yl)oxy)pyrimidin-2-yl)amino)phenyl)methanesulfonamide. The testing system contains 300ng/ml of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5ul of stop solution is added to stop the reaction. The KDR Kinase inhibition activity of a test compound is calculated based on the method recommended by the manufacturer. The IC50 values of the KDR kinase inhibition activity are calculated using XLfit software[1].
细胞实验	A CHO cellline stably transfected with hEGR cDNA and expressing hERG channels is used for the study.Whole-cell recording are performed using a 700B. Test compound is prepared as a 10 mM DMSO stock solution in a glass vial and is diluted using External Solution, the dilution is prepared no longer than 30 minutes before use. After achieving whole-cell configuration, the cells are monitored for 90 seconds to assess stability and washed with external solution for 66 sec. External solution containing 0.1% DMSO (vehicle) is applied to the cells to establish the baseline. After allowing the current to stabilize for 3 min, the test compound is applied. The test solution is added in 4 steps and the cells are kept in the test solution until the compound is effect reached a steady state or for a maximum of 6 min. Subsequently, the positive control (10 nM cisapride) is added. Washout with external solution is performed until the recovery of the current reached a steady state[1].
动物实验	The phamacokinetics of the test componds are studied with male ICR mice (n=6 for each group, weight 20-30 g) after a single intraveneous and oral dosing at 2.5 and 10 mg/kg, respectively. For i.v. dosing formulation, the test compound is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1 mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard.\

别名	KDR-IN-1, 索凡替尼
分子量	480.58
分子式	C24H28N6O3S
CAS No.	1308672-74-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Sulfatinib 1308672-74-3 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors VEGFR FGFR HER KDR-IN-1 索凡替尼 Inhibitor inhibitor inhibit

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Sulfatinib

存储

溶解度

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords