Cat. No.: HY-128589

CHMFL-KIT-033

Name: CHMFL-KIT-033
Brand: MedChemExpress
SKU: HY-128589
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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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Pureté : 99.74%
CAS No.: 2351801-41-5
Formule: C₂₃H₁₈FN₅O₂
Masse moléculaire:415.42

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CHMFL-KIT-033 Chemical Structure

CAS No.: 2351801-41-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Protocole (1)
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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 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	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	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	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	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	1 μM 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	>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]
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]
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]

Chemical Information

CAS No. 2351801-41-5
Appearance Solid
Masse moléculaire 415.42
Formule C₂₃H₁₈FN₅O₂
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (240.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4072 mL

12.0360 mL

24.0720 mL

5 mM

0.4814 mL

2.4072 mL

4.8144 mL

10 mM

0.2407 mL

1.2036 mL

2.4072 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (12.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (270 KB)
SDS (251 KB)
- English - EN (251 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

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CHMFL-KIT-033