2. Protein Tyrosine Kinase/RTK
  3. c-Kit
  4. CHMFL-KIT-033

CHMFL-KIT-033 是一种有效、可选择性的 c-KIT T670I 突变型的抑制剂, IC50 值为 0.045 μM。用于胃肠道间质瘤 (GISTs) 的研究。

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CHMFL-KIT-033

CHMFL-KIT-033 Chemical Structure

CAS No. : 2351801-41-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4442
In-stock
1 mg ￥1900
In-stock
5 mg ￥4860
In-stock
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Customer Review

CHMFL-KIT-033 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM[1].

IC50 & Target

IC50: 0.045 μM (c-KIT T670I mutant)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 EC50
1000 nM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused wild type c-KIT (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y823 residue after 2 hrs by Western blot analysis
Inhibition of TEL fused wild type c-KIT (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y823 residue after 2 hrs by Western blot analysis
[PMID: 31046271]
BaF3 EC50
34 nM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused wild type c-KIT T670I mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y823 residue after 2 hrs by Western blot analysis
Inhibition of TEL fused wild type c-KIT T670I mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y823 residue after 2 hrs by Western blot analysis
[PMID: 31046271]
BaF3 EC50
750 nM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused wild type c-KIT T670I mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y719 residue after 2 hrs by Western blot analysis
Inhibition of TEL fused wild type c-KIT T670I mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y719 residue after 2 hrs by Western blot analysis
[PMID: 31046271]
BaF3 EC50
77 nM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused wild type c-KIT T670I mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y703 residue after 2 hrs by Western blot analysis
Inhibition of TEL fused wild type c-KIT T670I mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y703 residue after 2 hrs by Western blot analysis
[PMID: 31046271]
BaF3 EC50
> 1000 nM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused wild type c-KIT (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y703 residue after 2 hrs by Western blot analysis
Inhibition of TEL fused wild type c-KIT (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y703 residue after 2 hrs by Western blot analysis
[PMID: 31046271]
BaF3 EC50
> 1000 nM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused wild type c-KIT (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y719 residue after 2 hrs by Western blot analysis
Inhibition of TEL fused wild type c-KIT (unknown origin) transfected in mouse BaF3 cells assessed as reduction in phosphorylation at Y719 residue after 2 hrs by Western blot analysis
[PMID: 31046271]
BaF3 GI50
0.008 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.026 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.031 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.044 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.122 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.157 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.265 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.525 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
0.868 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
1.15 μM
Compound: 24; CHMFL-KIT-033
Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
270 nM
Compound: 5
Growth inhibition of mouse BaF3 cells harboring TEL-VEGFR2 incubated for 72 hrs by CCK-8 assay
Growth inhibition of mouse BaF3 cells harboring TEL-VEGFR2 incubated for 72 hrs by CCK-8 assay
[PMID: 39353237]
BaF3 GI50
3.46 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
3.97 μM
Compound: 24; CHMFL-KIT-033
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
6 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
6.06 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
6.84 μM
Compound: 24; CHMFL-KIT-033
Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
[PMID: 31046271]
BaF3 GI50
> 10000 nM
Compound: 5
Growth inhibition of mouse BaF3 incubated for 72 hrs by CCK-8 assay
Growth inhibition of mouse BaF3 incubated for 72 hrs by CCK-8 assay
[PMID: 39353237]
GIST882 GI50
0.296 μM
Compound: 24; CHMFL-KIT-033
Antiproliferative activity against human GIST882 cells harboring c-KIT K642E mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human GIST882 cells harboring c-KIT K642E mutant incubated for 72 hrs by CCK8 assay
[PMID: 31046271]
GISTT1 GI50
0.052 μM
Compound: 24; CHMFL-KIT-033
Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant incubated for 72 hrs by CCK8 assay
[PMID: 31046271]
GISTT1 GI50
0.288 μM
Compound: 24; CHMFL-KIT-033
Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I double mutant incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I double mutant incubated for 72 hrs by CCK8 assay
[PMID: 31046271]
Sf9 IC50
45 nM
Compound: 24; CHMFL-KIT-033
Inhibition of His-tagged c-KIT T670I mutant (544 to 935 residues) (unknown origin) expressed in baculovirus infected sf9 cells pre-incubated for 60 mins followed by ATP addition and measured after 1 hr by Z-LYTE assay
Inhibition of His-tagged c-KIT T670I mutant (544 to 935 residues) (unknown origin) expressed in baculovirus infected sf9 cells pre-incubated for 60 mins followed by ATP addition and measured after 1 hr by Z-LYTE assay
[PMID: 31046271]
Sf9 IC50
536 nM
Compound: 24; CHMFL-KIT-033
Inhibition of wild-type His-tagged c-KIT (unknown origin) expressed in baculovirus infected sf9 cells pre-incubated for 60 mins followed by ATP addition and measured after 1 hr by Z-LYTE assay
Inhibition of wild-type His-tagged c-KIT (unknown origin) expressed in baculovirus infected sf9 cells pre-incubated for 60 mins followed by ATP addition and measured after 1 hr by Z-LYTE assay
[PMID: 31046271]
分子量

415.42

Formula

C23H18FN5O2
CAS 号
性状

固体

颜色

Light yellow to yellow

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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (240.72 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 2.4072 mL 12.0360 mL 24.0720 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 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

动物实验：

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: ≥ 5 mg/mL (12.04 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (12.04 mM); 澄清溶液

    此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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

只
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
参考文献

CHMFL-KIT-033 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4072 mL 12.0360 mL 24.0720 mL 60.1801 mL
5 mM 0.4814 mL 2.4072 mL 4.8144 mL 12.0360 mL
10 mM 0.2407 mL 1.2036 mL 2.4072 mL 6.0180 mL
15 mM 0.1605 mL 0.8024 mL 1.6048 mL 4.0120 mL
20 mM 0.1204 mL 0.6018 mL 1.2036 mL 3.0090 mL
25 mM 0.0963 mL 0.4814 mL 0.9629 mL 2.4072 mL
30 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0060 mL
40 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5045 mL
50 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2036 mL
60 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0030 mL
80 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7523 mL
100 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.6018 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.

Keywords:

CHMFL-KIT-0332351801-41-5c-KitSCFRCD117Inhibitorinhibitorinhibit

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