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

MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.

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

MET kinase-IN-2 Chemical Structure

MET kinase-IN-2 Chemical Structure

CAS No. : 2101241-90-9

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5 mg USD 260 In-stock
10 mg USD 410 In-stock
25 mg USD 780 In-stock
50 mg USD 1250 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity[1].

In Vitro

MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM[1].
MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM[1].

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

In Vivo

MET kinase-IN-2 (3-37.5 mg/kg; p.o.; 7 days per week for 3 weeks) exhibits statistically significant tumor growth inhibition in the U-87 MG 24 xeograft model[1].
MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2,CL, and F% values are 1.5 µg/mL, 10.7 µg•h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively[1].

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

Animal Model: 4-6 weeks old Female nude mice (U-87 MG xenograft model)[1]
Dosage: 3, 6, 12.5, 37.5 mg/kg
Administration: P.o.; 7 days per week for 3 weeks
Result: Induced dose-dependent tumor growth inhibition.
Animal Model: Male SD rats[1]
Dosage: 5 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: Displayed favorable overall PK profiles, with maximal plasma concentration (Cmax=1.5 µg/mL, 5-fold higher to that of IV), plasma exposure (AUC0-∞=10.7 µg•h/mL, 9.7-fold higher to that of IV), half-life (T1/2=4.9 h, 4.9-fold longer to that of IV), total clearance CL (0.5 L/h/kg; 10-fold lower to that of IV), and oral bioavailability (F=32%, 2.7-fold higher to that of IV) after oral dose of 5 mg/kg (10 mg/kg for IV).
Molecular Weight

562.59

Formula

C33H27FN4O4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C(C2=CC=CC=C2)=CNC3=C1C(NC4=CC=C(OC5=CC=NC6=CC(OCC(C)(O)C)=CC=C56)C(F)=C4)=NC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (177.75 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 1.7775 mL 8.8875 mL 17.7749 mL
5 mM 0.3555 mL 1.7775 mL 3.5550 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 (protect from light, stored under nitrogen). 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
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 (protect from light, stored under nitrogen). 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 1.7775 mL 8.8875 mL 17.7749 mL 44.4373 mL
5 mM 0.3555 mL 1.7775 mL 3.5550 mL 8.8875 mL
10 mM 0.1777 mL 0.8887 mL 1.7775 mL 4.4437 mL
15 mM 0.1185 mL 0.5925 mL 1.1850 mL 2.9625 mL
20 mM 0.0889 mL 0.4444 mL 0.8887 mL 2.2219 mL
25 mM 0.0711 mL 0.3555 mL 0.7110 mL 1.7775 mL
30 mM 0.0592 mL 0.2962 mL 0.5925 mL 1.4812 mL
40 mM 0.0444 mL 0.2222 mL 0.4444 mL 1.1109 mL
50 mM 0.0355 mL 0.1777 mL 0.3555 mL 0.8887 mL
60 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7406 mL
80 mM 0.0222 mL 0.1111 mL 0.2222 mL 0.5555 mL
100 mM 0.0178 mL 0.0889 mL 0.1777 mL 0.4444 mL
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MET kinase-IN-2 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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MET kinase-IN-2
Cat. No.:
HY-131065
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