Catalog No.S1361

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.

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MGCD-265 Chemical Structure

MGCD-265 Chemical Structure
Molecular Weight: 517.60

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Product Information

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  • Research Area
  • Inhibition Profile

Product Description

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]

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IC50 1 nM 2 nM 3 nM 3 nM
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]
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]

Protocol(Only for Reference)

Cell Assay: [2]

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.

Animal Study: [2]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Bonfils C. et al. AACR 2012 Annual Meeting, 2012. Abstract 1790.

[2] Beaulieu N. et al. 20th EORTC-NCI-AACR Symposium, 2008.

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02544633 Recruiting Non-Small Cell Lung Cancer Mirati Therapeutics Inc. October 2015 Phase 2
NCT01930006 Completed Advanced Malignancies Mirati Therapeutics Inc. August 2013 Phase 1
NCT00975767 Terminated Advanced Malignancies, Non-small Cell Lung Cancer Mirati Therapeutics Inc. August 2009 Phase 1
NCT00697632 Recruiting Advanced Cancer Mirati Therapeutics Inc. June 2008 Phase 1
NCT00679133 Completed Advanced Malignancies Mirati Therapeutics Inc. April 2008 Phase 1

Chemical Information

Download MGCD-265 SDF
Molecular Weight (MW) 517.60


CAS No. 875337-44-3
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 104 mg/mL (200.92 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-​[[[3-​fluoro-​4-​[[2-​(1-​methyl-​1H-​imidazol-​4-​yl)​thieno[3,​2-​b]​pyridin-​7-​yl]​oxy]​phenyl]​amino]​thioxomethyl]​-benzeneacetamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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