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MGCD-265_Molecular_structure_CAS_875337-44-3)
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MGCD-265

Catalog No. S1361 Name Selleck Chemicals
CAS Number 875337-44-3 Website http://www.selleckchem.com
M. F. C26H20FN5O2S2 Telephone (877) 796-6397
M. W. 517.5977032 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 72634

SYNONYMS

IUPAC name
1-(3-fluoro-4-{[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-3-(2-phenylacetyl)thiourea
IUPAC Traditional name
1-(3-fluoro-4-{[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)-3-(2-phenylacetyl)thiourea

DATABASE IDS

CAS Number 875337-44-3

PROPERTIES

Target Met
Target VEGFR
Target Tie-2
Salt Data Free Base
Solubility DMSO
Storage Condition -20°C

DETAILS

Description (English)
Research Area
Description Solid tumours,Non-small cell lung cancer
Biological Activity
Description MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of Met, VEGFR1, VEGFR2, VEGFR3, Ron, and Tie2 with IC50 of 1 nM, 3 nM, 3 nM, 4 nM, 2 nM and 7 nM, respectively.
Targets Met VEGFR1 VEGFR2 VEGFR3 Ron Tie2
IC50 1 nM 3 nM 3 nM 4 nM 2 nM 7 nM [1]
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]
Clinical Trials A Phase I clinical trial of MGCD-265 in advanced malignancies has been completed. Currently, MGCD-265, in combination of erlotinib or docetaxel, is under investigation in a Phase I/II clinical trial for advanced malignancies or non-small cell lung cancer.
Features
Protocol
Cell Assay [2]
Cell Lines HCT116, MDA-MB-231, SNU-5, and MKN45 cells
Concentrations 0–5 μM
Incubation Time 72 hours
Methods 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
Doses 20 mg/kg–60 mg/kg
Administration Orally
References
[1] Bonfils C. et al. AACR 2012 Annual Meeting, 2012. Abstract 1790.
[2] Beaulieu N. et al. 20th EORTC-NCI-AACR Symposium, 2008.