MGCD-265

  Cat. No.:  DC7462  
Chemical Structure
875337-44-3
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More than 5000 active chemicals with high quality for research!
Field of application
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2.
Cas No.: 875337-44-3
Synonyms: MGCD 265; MGCD265
SMILES: O=C(CC1=CC=CC=C1)NC(NC2=CC=C(C(F)=C2)OC3=C4C(C=C(S4)C5=CN(C=N5)C)=NC=C3)=S
Formula: C26H20FN5O2S2
M.Wt: 517.6
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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. 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. For the detailed information of MGCD-265, the solubility of MGCD-265 in water, the solubility of MGCD-265 in DMSO, the solubility of MGCD-265 in PBS buffer, the animal experiment (test) of MGCD-265, the cell expriment (test) of MGCD-265, the in vivo, in vitro and clinical trial test of MGCD-265, the EC50, IC50,and Affinity of MGCD-265, Please contact DC Chemicals.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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