MGCD-265 analog

SKU: orb1300844

Description

MGCD-265 analog

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 875337-44-3
• MW: 517.6
• Purity: 98.06% (May vary between batches)
• Formula: C₂₆H₂₀FN₅O₂S₂
• SMILES: Cn1cnc(c1)-c1cc2nccc(Oc3ccc(NC(=S)NC(=O)Cc4ccccc4)cc3F)c2s1
• Target: Apoptosis,c-Met/HGFR,VEGFR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.38 mM);DMSO:96 mg/mL (185.47 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  c-Met:29 nM|VEGFR2:10 nM
• In Vivo:
  In c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87 mg, 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 U87 mg xenograft. MGCD-265 also inhibits the plasma level of shed-Met.
• 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. 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.
• Cell Research:
  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)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-Met, c-Met/HGFR, cMet/HGFR, cMet, Apoptosis, angiogenesis, kinases, invasion, morphogenesis, MGCD 265, MGCD 265 analog, MGCD265, MGCD265 analog, MGCD-265 analog, Met, migration, HGFR, Glesatinib, Glesatinib analog, proliferation, RON, survival, tyrosine, VEGFR3, VEGFR, VEGFR1, VEGFR2

Compound Identifiers

PubChem CID

24901704