MGCD-265 analog

Name: MGCD-265 analog
Brand: Selleck Chemicals
SKU: S1361
Rating: 5 (7 reviews)

For research use only.

Catalog No.S1361

7 publications

Molecular Weight(MW): 517.60

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.

Selleck's MGCD-265 analog has been cited by 7 publications

Protein Cell, 2019, 10(3):161-177

PubMed: 29667003 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(7):1526-1539

PubMed: 29654068 ( click the link to review the publication )

PLoS One, 2018, 13(4):e0194730

PubMed: 29641535 ( click the link to review the publication )

Am J Physiol Lung Cell Mol Physiol, 2017, 312(6):L861-L872

PubMed: 28336813 ( click the link to review the publication )

Cancer Discov, 2016, 6(12):1334-1341

PubMed: 27694386 ( click the link to review the publication )

Cancer Lett, 2013, 340(1):43-50

PubMed: 23811285 ( click the link to review the publication )

Int J Clin Exp Pathol, 2013, 6(10):2082-91

PubMed: 24133586 ( click the link to review the publication )

3 Customer Reviews

c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.

Cancer Lett 2013 340(1), 43-50. MGCD-265 analog purchased from Selleck.

Western blot analysis of c-Met and p-c-Met. 0-5 μM MGCD265 was added.

Dr. Zhang of Tianjin Medical University. MGCD-265 analog purchased from Selleck.
Immunoblot analysis for FRS2, AKT, and ERK activity for NCI-H2077 cells treated for 48 hours with DMSO, BGJ398, or additional kinase inhibitors as indicated, or combination treatment as indicated (Tram, trametinib; LDC, LDC1267; LOXO, LOXO-101; Imat, imatinib; MGCD, MGCG-265).

Mol Cancer Ther, 2018, 17(7):1526-1539. MGCD-265 analog purchased from Selleck.

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]	View More
1 nM	2 nM	3 nM	3 nM	4 nM	View More

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	M2rTfGZ2dmO2aX;uJIF{e2G7				NIS1[GFKdmirYnn0bY9vKG:oIFfTWEB1[WepZXSgWmVITlJ{IHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NE4xOSEQvF2=	M{W3flE5PDN2MUS1
293T cells	M{[4bWZ2dmO2aX;uJIF{e2G7				NVvWc24yUW6qaXLpeIlwdiCxZjDUVHIu\nW\|ZXSgUYV1KHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhcW5iaIXtZY4hOjl\|VDDj[YxteyCkeTDFUGlUSSxiSVO1NF0xNjB3IN88US=>	M3S4[lE6OjFzMkS5

... 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

Cell Research: ^[2]	- Collapse 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. (Only for Reference)
Animal Research: ^[2]	- Collapse 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 (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	104 mg/mL (200.92 mM)
	Water	Insoluble
	Ethanol	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 Information Download MGCD-265 analog SDF

Molecular Weight	517.60
Formula	C₂₆H₂₀FN₅O₂S₂
CAS No.	875337-44-3
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	C[N]1C=NC(=C1)C2=CC3=NC=CC(=C3S2)OC4=CC=C(NC(=S)NC(=O)CC5=CC=CC=C5)C=C4F

In vivo Formulation Calculator (Clear solution)

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

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

Bio Calculators

Molarity Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Computed Result

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C3=C2/X	C3:	LOG(C3):
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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

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

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c-Met Signaling Pathway Map

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MGCD-265 analog