Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MGCD-265 analog (Glesatinib) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 51.00 | |
2 mg | In stock | $ 71.00 | |
5 mg | In stock | $ 116.00 | |
10 mg | In stock | $ 209.00 | |
25 mg | In stock | $ 348.00 | |
50 mg | In stock | $ 518.00 | |
100 mg | In stock | $ 753.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 143.00 |
Description | MGCD-265 analog (Glesatinib) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively. |
Targets&IC50 | c-Met:29 nM, VEGFR2:10 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. |
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. |
Kinase Assay | Time-resolved fluorescence resonance energy transfer assay: The c-Met–catalyzed phosphorylation of N-biotinylated peptide (EQEDEPEGDYFEWLE-CONH2) is measured using a time-resolved fluorescence resonance energy transfer assay. [2] The MK-2461 IC50 for Ron, Mer, Flt1, Flt3, Flt4, KDR, PDGFRβ, FGFR1, FGFR2, FGFR3, TrkA, and TrkB are determined using time-resolved fluorescence resonance energy transfer assays similar to the c-Met kinase assay. |
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) |
Synonyms | MGCD-265, Glesatinib |
Molecular Weight | 517.6 |
Formula | C26H20FN5O2S2 |
CAS No. | 875337-44-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 96 mg/mL (185.5 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
MGCD-265 analog 875337-44-3 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors VEGFR c-Met/HGFR cell MGCD-265 angiogenesis kinases Glesatinib MGCD265 proliferation Inhibitor MGCD 265 morphogenesis invasion MGCD265 analog Vascular endothelial growth factor receptor inhibit survival MGCD 265 analog migration receptor tyrosine inhibitor