1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR VEGFR
  3. MET kinase-IN-4

MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer.

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

MET kinase-IN-4 Chemical Structure

MET kinase-IN-4 Chemical Structure

CAS No. : 888719-03-7

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5 mg USD 195 In-stock
10 mg USD 310 In-stock
25 mg USD 580 In-stock
50 mg USD 850 In-stock
100 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer[1].

IC50 & Target

IC50: 1.9 nM (Met); 4 nM (Flt-3); 27 nM (VEGFR-2)[1]

In Vitro

MET kinase-IN-4 (Compound 2) has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM[1].
MET kinase-IN-4 inhibits Flt-3 and VEGFR-2 kinases with IC50 values of 4 and 27 nM, respectively[1].
MET kinase-IN-4 (3 μM) shows good metabolic stability in both human and mouse liver microsomes[1].

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

In Vivo

MET kinase-IN-4 (Compound 2) (i.v., p.o.; 5, 10 mg/kg) possesses a favorable pharmacokinetic profile in mice[1].
MET kinase-IN-4 (p.o.; 6.25, 12.5, 25 and 50 mg/kg; once a day) demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model[1].

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

Animal Model: Mice[1]
Dosage: 5, 10 mg/kg
Administration: IV, PO
Result: Showed extensive extravascular distribution and a favorable half-life.
Animal Model: Nude mice[1]
Dosage: 6.25, 12.5, 25 and 50 mg/kg
Administration: PO, once a day
Result: Showed antitumor activity in dose-dependet.
Molecular Weight

458.42

Formula

C25H16F2N4O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=CN(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NC=C5)=NC=C4)C(F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (218.14 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 2.1814 mL 10.9070 mL 21.8141 mL
5 mM 0.4363 mL 2.1814 mL 4.3628 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.45 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

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). 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 2.1814 mL 10.9070 mL 21.8141 mL 54.5351 mL
5 mM 0.4363 mL 2.1814 mL 4.3628 mL 10.9070 mL
10 mM 0.2181 mL 1.0907 mL 2.1814 mL 5.4535 mL
15 mM 0.1454 mL 0.7271 mL 1.4543 mL 3.6357 mL
20 mM 0.1091 mL 0.5454 mL 1.0907 mL 2.7268 mL
25 mM 0.0873 mL 0.4363 mL 0.8726 mL 2.1814 mL
30 mM 0.0727 mL 0.3636 mL 0.7271 mL 1.8178 mL
40 mM 0.0545 mL 0.2727 mL 0.5454 mL 1.3634 mL
50 mM 0.0436 mL 0.2181 mL 0.4363 mL 1.0907 mL
60 mM 0.0364 mL 0.1818 mL 0.3636 mL 0.9089 mL
80 mM 0.0273 mL 0.1363 mL 0.2727 mL 0.6817 mL
100 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5454 mL
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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.

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Product Name:
MET kinase-IN-4
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HY-18309
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