| CAS NO: | 875337-44-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 517.60 |
|---|---|
| Formula | C26H20FN5O2S2 |
| CAS No. | 875337-44-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 104 mg/mL (200.9 mM) |
| Water: <1 mg/mL | |
| Ethanol:<1 mg/mL | |
| Solubility (In vivo) | Chemical Name: N-((3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide InChi Key: UFICVEHDQUKCEA-UHFFFAOYSA-N InChi Code: InChI=1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35) SMILES Code: O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=CN(C)C=N4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=CC=C5 |
| Synonyms | MGCD265-analog; Glesatinib-analog; MGCD-265-analog; MGCD 265-analog; |
| In Vitro | In vitro activity: MGCD-265 analog is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 analog potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. MGCD-265 analog 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 analog(40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 analog (6 nM–1 μM) also induces apoptosis in MKN45 cells Kinase Assay: MGCD-265-analog (structurally related to MGCD-265) 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. IC50 value:10 nM (VEGFR2), 29 nM(c-Met) Cell Assay: Cells (HCT116, MDA-MB-231, SNU-5, and MKN45 cells) are treated with MGCD-265 analog for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours. |
|---|---|
| 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 analog (20 mg/kg–60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 analog (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 analog also inhibits the plasma level of shed-Met. |
| Animal model | Mice |
| Formulation & Dosage | 20–60 mg/kg |
| References | J. M. Besterman, M. Fournel, I. Dupont, C. Bonfils, M. Dubay, H. Ste-Croix, C. R. Maroun; MethylGene, Inc., Montreal, QC, Canada, Potent preclinical antitumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib, J Clin Oncol 28, 2010 (suppl; abstr e13595). |
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