MGCD-265 analog

Catalog No.S1361

For research use only.

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

CAS No. 875337-44-3

Selleck's MGCD-265 analog has been cited by 12 Publications

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Purity & Quality Control

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells M1PySGZ2dmO2aX;uJIF{e2G7 M33SVWlvcGmkaYTpc44hd2ZiR2PUJJRi\2enZDDWSWdHWjJiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{whUUN3ME2wMlAyKM7:TR?= NWnVTG57OTh2M{SxOFU>
293T cells M4L1emZ2dmO2aX;uJIF{e2G7 M{nUVWlvcGmkaYTpc44hd2ZiVGDSMYZ2e2WmIF3leEBxcG:|cHjvdplt[XSrb36g[ZhxemW|c3XkJIlvKGi3bXHuJFI6O1RiY3XscJMh[nliRVzJV2EtKEmFNUC9NE4xPSEQvF2= MUWxPVIyOTJ2OR?=
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 (from reference)

Cell Research:

[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 Research:

[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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 517.60
Formula

C26H20FN5O2S2

CAS No. 875337-44-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02544633 Completed Drug: MGCD265 Non-Small Cell Lung Cancer Mirati Therapeutics Inc. October 2015 Phase 2
NCT01930006 Completed Drug: MGCD265 Advanced Malignancies Mirati Therapeutics Inc. August 2013 Phase 1
NCT02117245 Completed -- Healthy Mirati Therapeutics Inc. December 2011 --
NCT00975767 Terminated Drug: MGCD265+erlotinib|Drug: MGCD265+docetaxel Advanced Malignancies Non-small Cell Lung Cancer Mirati Therapeutics Inc. August 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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