Home Protein Tyrosine Kinase c-Met inhibitor - Tie-2 inhibitor - VEGFR inhibitor - RON inhibitor MGCD-265 analog For research use only.

MGCD-265 analog

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.

MGCD-265 analog Chemical Structure

MGCD-265 analog Chemical Structure

CAS No. 875337-44-3

Purity & Quality Control

MGCD-265 analog Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Function assay Inhibition of GST tagged VEGFR2 expressed in Sf9 cells, IC50=0.01 μM 18434145
293T cells Function assay Inhibition of TPR-fused Met phosphorylation expressed in human 293T cells by ELISA, IC50=0.05 μM 19211249
Click to View More Cell Line Experimental Data

Biological Activity

Description MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.
Targets
Met [1] RON [1] VEGFR1 [1] VEGFR2 [1] VEGFR3 [1] Click to View More Targets
1 nM 2 nM 3 nM 3 nM 4 nM
In vitro
In vitro MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. [1] MGCD-265 inhibits cell proliferation both in c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and in non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), with IC50 values of 6 nM–30 nM and 1 μM–3 μM, respectively. In serum starved MKN45 cells, MGCD-265 (40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 (6 nM–1 μM) also induces apoptosis in MKN45 cells. [2]
Cell Research Cell lines HCT116, MDA-MB-231, SNU-5, and MKN45 cells
Concentrations 0–5 μM
Incubation Time 72 hours
Method

Cells are treated with MGCD-265 for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours.
In Vivo
In vivo In c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 tumor cells, MGCD-265 (20 mg/kg–60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 (40 mg/kg) also downregulates genes involved in angiogenesis, including VEGF and IL-8, both in tumor and plasma of mice with U87MG xenograft. MGCD-265 also inhibits the plasma level of shed-Met. [2]
Animal Research Animal Models Mice (CD-1 nude) xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 cells
Dosages 20 mg/kg–60 mg/kg
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02544633 Completed
Non-Small Cell Lung Cancer
Mirati Therapeutics Inc.
 October 2015 Phase 2
NCT01930006 Completed
Advanced Malignancies
Mirati Therapeutics Inc.
 August 2013 Phase 1
NCT02117245 Completed
Healthy
Mirati Therapeutics Inc.
 December 2011 --
NCT00975767 Terminated
Advanced Malignancies Non-small Cell Lung Cancer
Mirati Therapeutics Inc.
 August 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 517.60 Formula

C26H20FN5O2S2
CAS No. 875337-44-3 SDF Download MGCD-265 analog SDF
Smiles CN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 104 mg/mL ( (200.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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