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MGCD-265 analog

Name: MGCD-265 analog
Brand: Selleck Chemicals
SKU: S1361
Rating: 5 (12 reviews)

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.

CAS No. 875337-44-3

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

3 Customer Reviews

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c-Met Signaling Pathway Map

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	Click to View More Targets

In vitro

MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, Met^Y1235D, Met^M1250T, 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?=

Click to View More Cell Line Experimental Data

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

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	517.60
Formula	C₂₆H₂₀FN₅O₂S₂
CAS No.	875337-44-3
Storage	3 years	-20°C	powder
Storage	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

Download MGCD-265 analog SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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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.

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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