1. Protein Tyrosine Kinase/RTK
  2. c-Kit c-Met/HGFR
  3. c-Kit-IN-1

c-Kit-IN-1 是一种有效的 c-Kitc-Met 抑制剂,IC50 值 <200 nM。

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c-Kit-IN-1 Chemical Structure

c-Kit-IN-1 Chemical Structure

CAS No. : 1225278-16-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1180
In-stock
5 mg ¥1100
In-stock
10 mg ¥1800
In-stock
25 mg ¥3900
In-stock
50 mg ¥7000
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100 mg   询价  
200 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.

IC50 & Target

IC50: <200 nM (c-Met), <200 nM (c-Kit), <2 μM (KDR), <10 μM (PDGFRα), <10 μM (PDGFRβ)[1]

体外研究
(In Vitro)

c-Kit-IN-1 is a c-Kit and c-Met inhibitor extracted from patent 2010051373A1, compound example 45, has an IC50 of <200 nM. c-Kit-IN-1 also inhibits KDR, PDGFR α and β with IC50s of <2 μM, <10 μM and <10 μM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

489.47

Formula

C26H21F2N5O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (204.30 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0430 mL 10.2151 mL 20.4303 mL
5 mM 0.4086 mL 2.0430 mL 4.0861 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.11 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.11 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.83%

参考文献
Kinase Assay
[1]

Activity of c-KIT kinase is determined by following the production of ADP from the kinase reaction through coupling with the pyruvate kinase/lactate dehydrogenase system. In this assay, the oxidation of NADH (thus the decrease at A340nm) is continuously monitored spectrophometrically. The reaction mixture (100 μL) contained c-KIT (cKIT residues T544-V976, from ProQinase, 5.4 nM), polyE4Y (1 mg/mL), MgC12 (10 mM), pyruvate kinase (4 units), lactate dehydrogenase (0.7 units), phosphoenol pyruvate (1 mM), and NADH (0.28 mM) in 90 mM Tris buffer containing 0.2 % octyl-glucoside and 1% DMSO, pH 7.5. Test compounds (e.g., c-Kit-IN-1) are incubated with c-KIT and other reaction reagents at 22°C for <2 min before ATP (200 μM) is added to start the reaction. The absorption at 340 nm is monitored continuously for 0.5 hours at 30°C on Polarstar Optima plate reader (BMG). The reaction rate is calculated using the 0 to 0.5 h time frame. Percent inhibition is obtained by comparison of reaction rate with that of a control (i.e. with no test compound). IC50 values are calculated from a series of percent inhibition values determined at a range of inhibitor concentrations using software routines as implemented in the GraphPad Prism software package[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

A serial dilution of test compounds (e.g., c-Kit-IN-1) are dispensed into a 96-well black clear bottom plate. For each cell line, five thousand cells are added per well in 200 μL complete growth medium. Plates are incubated for 67 hours at 37 degrees Celsius, 5% CO2, 95% humidity. At the end of the incubation period 40 μL of a 440 μM solution of resazurin in PBS is added to each well and incubated for an additional 5 hours at 37 degrees Celsius, 5% CO2, 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nM and an emission of 600 nM. Data is analyzed using Prism software to calculate IC50 values[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

c-Kit-IN-1 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0430 mL 10.2151 mL 20.4303 mL 51.0757 mL
5 mM 0.4086 mL 2.0430 mL 4.0861 mL 10.2151 mL
10 mM 0.2043 mL 1.0215 mL 2.0430 mL 5.1076 mL
15 mM 0.1362 mL 0.6810 mL 1.3620 mL 3.4050 mL
20 mM 0.1022 mL 0.5108 mL 1.0215 mL 2.5538 mL
25 mM 0.0817 mL 0.4086 mL 0.8172 mL 2.0430 mL
30 mM 0.0681 mL 0.3405 mL 0.6810 mL 1.7025 mL
40 mM 0.0511 mL 0.2554 mL 0.5108 mL 1.2769 mL
50 mM 0.0409 mL 0.2043 mL 0.4086 mL 1.0215 mL
60 mM 0.0341 mL 0.1703 mL 0.3405 mL 0.8513 mL
80 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6384 mL
100 mM 0.0204 mL 0.1022 mL 0.2043 mL 0.5108 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
c-Kit-IN-1
目录号:
HY-15240
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