Find C-Met Inhibitors, ARQ 197 Inhibitor, Tivantinib Inhibitor on Industry Directory, Reliable Manufacturer/Supplier/Factory from China.

Inquiry Basket (0)

MK-2461 917879-39-1

Product Description

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

495.55 MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2.
.


Biological Activity


MK-2461 also potently inhibits FGFR1, FGFR2, FGFR3, KDR, TrkA, TrkB, and
Flt4 with IC50 of 65 nM, 39 nM, 50 nM, 44 nM, 46 nM, 61 nM, and 78 nM,
respectively. Compared with wild-type c-Met, MK-2461 more potently
inhibits the activity of oncogenic c-Met kinase mutants such as N1100Y,
Y1230C, Y1230H, Y1235D, and M1250T with IC50 of 1.5 nM, 1.5 nM, 1.0 nM,
0.5 nM, and 0.4 nM, respectively.


MK-2461 binds more strongly to
phosphorylated c-Met than to unphosphorylated c-Met. MK-2461 potently
inhibits ATP-induced autophosphorylation of the COOH-terminal docking
domain of c-Met, but not the activation loop. In contrast, MK-2461
inhibits phosphorylation of the activation loop of FGFR2 (Y653/Y654) in
Kato III cells and PDGFRα (Y849) in H1703 cells with IC50 of


MK-2461 treatment significantly inhibits c-Met (Y1349) phosphorylation
in GTL-16 tumors with IC50 of ~1 μM. Oral administration of MK-2461 at
10 mg/kg, 50 mg/kg, and 100 mg/kg twice daily as well as 200 mg/kg once
daily effectively suppresses tumor growth of GTL-16 xenografts in mice
by 62%, 77%, 75%, and 90%, respectively. Similarly, MK-2461 treatment at
134 mg/kg twice daily inhibits the growth of NIH3T3 tumors harboring
c-Met single nucleotide mutants T3936C and T3997C, by 78% and 62%,
respectively.






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. 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.

Contact us if you need more details on 917879-39-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about MK-2461 917879-39-1、917879-39-1 MK-2461. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Protein Tyrosine Kinase > c-Met Inhibitor