Cat. No.: HY-15240

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c-Kit-IN-1

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC₅₀s of <200 nM.

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Pureté: 98.26%
CAS No.: 1225278-16-9
Formule: C₂₆H₂₁F₂N₅O₃
Masse moléculaire:489.47

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

c-Kit-IN-1 Chemical Structure

CAS No.: 1225278-16-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC₅₀s of <200 nM.

IC₅₀ & Target

IC50: <200 nM (c-Met), <200 nM (c-Kit), <2 μM (KDR), <10 μM (PDGFRα), <10 μM (PDGFRβ)^[1]

In Vitro

c-Kit-IN-1 is a c-Kit and c-Met inhibitor extracted from patent 2010051373A1, compound example 45, has an IC₅₀ of <200 nM. c-Kit-IN-1 also inhibits KDR, PDGFR α and β with IC₅₀s of <2 μM, <10 μM and <10 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1225278-16-9
Appearance Solid
Masse moléculaire 489.47
Formule C₂₆H₂₁F₂N₅O₃
Color White to off-white
SMILES

O=C(C1(CC1)C(NC2=CC=CC=C2)=O)NC3=CC(F)=C(OC4=CC=NC(C5=CN(C)N=C5)=C4)C=C3F
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Cell Mol Gastroenterol Hepatol

Sorafenib Promotes Treg Cell Differentiation To Compromise Its Efficacy via VEGFR/AKT/Foxo1 Signaling in Hepatocellular Carcinoma. [Abstract]

2024 Dec 30:101454. PMID: 39743020
SSRN

2026 May 20.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (204.30 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

2.0430 mL

10.2151 mL

20.4303 mL

5 mM

0.4086 mL

2.0430 mL

4.0861 mL

10 mM

0.2043 mL

1.0215 mL

2.0430 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Kinase Assay^[1]

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 A340nm) is continuously monitored spectrophometrically. 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., c-Kit-IN-1) 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). IC₅₀ values are calculated from a series of percent inhibition values determined at a range of inhibitor concentrations using software routines as implemented in the GraphPad Prism software package^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

A serial dilution of test compounds (e.g., c-Kit-IN-1) are 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. Data is analyzed using Prism software to calculate IC₅₀ values^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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]. Daniel L. Flynn, et al. Cyclopropane amides and analogs exhibiting anti-cancer and anti-proliferative activities. WO 2010051373 A1

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0430 mL	10.2151 mL	20.4303 mL	51.0757 mL
	5 mM	0.4086 mL	2.0430 mL	4.0861 mL	10.2151 mL
	10 mM	0.2043 mL	1.0215 mL	2.0430 mL	5.1076 mL
	15 mM	0.1362 mL	0.6810 mL	1.3620 mL	3.4050 mL
	20 mM	0.1022 mL	0.5108 mL	1.0215 mL	2.5538 mL
	25 mM	0.0817 mL	0.4086 mL	0.8172 mL	2.0430 mL
	30 mM	0.0681 mL	0.3405 mL	0.6810 mL	1.7025 mL
	40 mM	0.0511 mL	0.2554 mL	0.5108 mL	1.2769 mL
	50 mM	0.0409 mL	0.2043 mL	0.4086 mL	1.0215 mL
	60 mM	0.0341 mL	0.1703 mL	0.3405 mL	0.8513 mL
	80 mM	0.0255 mL	0.1277 mL	0.2554 mL	0.6384 mL
	100 mM	0.0204 mL	0.1022 mL	0.2043 mL	0.5108 mL

Keywords

c-Kit-IN-1

2 Cited Publications

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c-Kit-IN-1

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

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FDA Approved & Pharmacopeial Drug Library

Anti-Lung Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) c-Kit-IN-1

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

c-Kit-IN-1 Related Classifications

HY-15240 Related Classifications