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MGCD-265 analog

Catalog No. T6351 CAS 875337-44-3

Synonyms: MGCD-265, Glesatinib

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.

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MGCD-265 analog, CAS 875337-44-3

Pack Size	Availability	Price/USD
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

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Purity: 99.21%

Purity: 98.06%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 96 mg/mL (185.5 mM)

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cardiovascular Disease Compound Library Anti-Liver Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Colorectal Cancer Compound Library

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Keywords

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

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