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c-Kit-IN-1

c-Kit-IN-1

产品编号 T4332   CAS 1225278-16-9
别名: PDGFR inhibitor 1, DCC-2618

c-Kit-IN-1 (DCC-2618) 是c-Kit 和c-Met 抑制剂(IC50<200 nM)。

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c-Kit-IN-1 Chemical Structure
c-Kit-IN-1, CAS 1225278-16-9
规格 价格/CNY 货期 数量
1 mg ¥ 378 现货
2 mg ¥ 548 现货
5 mg ¥ 898 现货
10 mg ¥ 1,490 现货
25 mg ¥ 3,230 现货
50 mg ¥ 4,770 现货
100 mg ¥ 6,780 现货
500 mg ¥ 13,600 待询
1 mL * 10 mM (in DMSO) ¥ 978 现货
其他形式的 c-Kit-IN-1:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: c-Kit-IN-1 (T4332)
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纯度: 98.72%
纯度: 98.16%
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生物活性
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存储 & 溶解度
参考文献
产品描述 c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).
靶点活性 c-Kit:<200 nM, c-Met:<200 nM
体外活性 DCC-2618 also inhibits KDR and PDGFR α/β (IC50s: <2 μM, <10 μM and <10 μM).
激酶实验 The 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 A340 nM) is continuously monitored spectrophotometrically. 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., DCC-2618) 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).
细胞实验 DCC-2618 is prepared in DMSO and stored, and then diluted with the appropriate medium before use.A serial dilution of test compounds (e.g., DCC-2618) is 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.
别名 PDGFR inhibitor 1, DCC-2618
分子量 489.47
分子式 C26H21F2N5O3
CAS No. 1225278-16-9

存储

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

溶解度

DMSO: 88 mg/mL(179.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.043 mL 10.2151 mL 20.4303 mL 51.0757 mL
5 mM 0.4086 mL 2.043 mL 4.0861 mL 10.2151 mL
10 mM 0.2043 mL 1.0215 mL 2.043 mL 5.1076 mL
20 mM 0.1022 mL 0.5108 mL 1.0215 mL 2.5538 mL
50 mM 0.0409 mL 0.2043 mL 0.4086 mL 1.0215 mL
100 mM 0.0204 mL 0.1022 mL 0.2043 mL 0.5108 mL

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TargetMol Library Books参考文献

1. Daniel L. Flynn, et al. Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities. WO 2010051373 A1
Ningetinib Tepotinib hydrochloride(1 : x) CSF1R-IN-2 PF-04217903 phenolsulfonate c-Met-IN-2 Rilotumumab CEP-40783 PHA-665752

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 药物功能重定位化合物库 激酶抑制剂库 抗癌上市药物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌药物库 抑制剂库 FDA 上市激酶抑制剂库 膜蛋白靶向化合物库

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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。

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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

c-Kit-IN-1 1225278-16-9 Tyrosine Kinase/Adaptors c-Met/HGFR c-Kit PDGFR inhibitor 1 CD117 DCC-2618 Inhibitor DCC 2618 DCC2618 cKitIN1 SCFR inhibit c Kit IN 1 inhibitor

 

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