MGCD-265

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

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

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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]
Features

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
Formulation
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)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
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

References

[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 http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
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
Formula

C26H20FN5O2S2

CAS No. 875337-44-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 104 mg/mL (200.92 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <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

Customer Product Validation(2)


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Rating
Source Cancer Lett 2013 340(1), 43-50. MGCD-265 purchased from Selleck
Method Western blotting
Cell Lines SK-BR-3-LR cells
Concentrations 0.1 uM
Incubation Time 48 h
Results As shown in Figure, crizotinib, a c-MET, RON and ALK kinase inhibitor, MGCD-265, a multi-targeted kinase inhibitor targeting c-MET, VEGFR1/2/3 and RON and XL880, a multi-targeted kinase inhibitor of c-MET, KDR, FLT3, PDGFR and RON, could significantly restore lapatinib sensitivity in SK-BR-3-LR cells when combined with lapatinib at a concentration of 0.1 uM. Consistent with the cell proliferation data, the Western blot results demonstrated that only crizotinib, MGCD-265 and XL880, but not sunitinib, TAE-684, and dasatinib, significantly inhibited AKT and ERK1/2 phosphorylation in SK-BR-3-LR cells when combined with lapatinib.

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Rating
Source Dr. Zhang of Tianjin Medical University. MGCD-265 purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 cells
Concentrations 0-5 μM
Incubation Time
Results MGCD-265 treatment resulted in a reduction of c-Met phosphorylation in MDA-MB-231 cells.

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.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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