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 Chemical Structure

CHMFL-KIT-033 Chemical Structure

CAS No. : 2351801-41-5

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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 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 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 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 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 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 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]
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
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CHMFL-KIT-033 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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