1. Protein Tyrosine Kinase/RTK
  2. c-Kit c-Met/HGFR
  3. c-Kit-IN-1

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

For research use only. We do not sell to patients.

c-Kit-IN-1 Chemical Structure

c-Kit-IN-1 Chemical Structure

CAS No. : 1225278-16-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 118 In-stock
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10 mM * 1 mL in DMSO USD 118 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 180 In-stock
25 mg USD 390 In-stock
50 mg USD 700 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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.

Molecular Weight

489.47

Formula

C26H21F2N5O3

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0430 mL 10.2151 mL 20.4303 mL
5 mM 0.4086 mL 2.0430 mL 4.0861 mL
View the Complete Stock Solution Preparation Table
  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.83%

References
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].

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].

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

References

Complete Stock Solution Preparation Table

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
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c-Kit-IN-1 Related Classifications

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.

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Product Name:
c-Kit-IN-1
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