CHMFL-KIT-033

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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.

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CHMFL-KIT-033 Chemical Structure

CAS No. : 2351801-41-5

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Description

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]

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]

Molecular Weight

415.42

Formula

C₂₃H₁₈FN₅O₂

CAS No.

2351801-41-5

SMILES

O=C(CC(NC1=CC=CC(F)=C1)=O)NC2=CC(NN=C3/C=C/C4=CC=CC=N4)=C3C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu X, et al. Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). J Med Chem. 2019 May 23;6 [Content Brief]

CHMFL-KIT-033 Related Classifications

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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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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