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

MET kinase-IN-2 

Cat. No.: HY-131065
Handling Instructions

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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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].

IC50 & Target[1]

MET

7.4 nM (IC50)

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].

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].

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.

2101241-90-9

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

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

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Keywords:

MET kinase-IN-2c-Met/HGFRselectiveoraltumorantiproliferativeU-87 MGcellsInhibitorinhibitorinhibit

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