MGCD-265 analog

Catalog No.S1361

MGCD-265 analog Chemical Structure

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.

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In DMSO USD 350 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Cited by 4 Publications

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]
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 NIDsXHdHfW6ldHnvckBie3OjeR?= MoTsTY5pcWKrdHnvckBw\iCJU2SgeIFo\2WmIG\FS2ZTOiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNFEh|ryP NEi2PHAyQDR|NEG0OS=>
293T cells NXPwW3pxTnWwY4Tpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKFSSUj3meZNm\CCPZYSgdIhwe3Cqb4L5cIF1cW:wIHX4dJJme3OnZDDpckBpfW2jbjCyPVNVKGOnbHzzJIJ6KEWOSWPBMEBKSzVyPUCuNFUh|ryP NYTHNG5OOTl{MUGyOFk>

... 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]
+ Expand
  • 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]
+ Expand
  • 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
    (Only for Reference)

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

Molecular Weight 517.60
Formula

C26H20FN5O2S2
CAS No. 875337-44-3
Storage powder
in solvent
Synonyms N/A

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c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID