All AbMole products are for research use only, cannot be used for human consumption.
MK-2461 is a potent inhibitor of c-Met, Ron, Flt1, Flt 3, PDGFRβ, and Mer with IC50 of 2.5 nM, 7 nM, 10 nM, 22 nM, 22 nM, and 24 nM, respectively. MK-2461 also exhibits significant activities toward several other kinases including 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. MK-2461 preferentially binds to the activated c-Met, and is slightly more potent against five naturally occurring oncogenic human c-Met mutants (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) compared with wild-type c-Met. MK-2461 significantly inhibits constitutive and ligand-induced phosphorylation of the juxtamembrane domain (Y1003) and the COOH-terminal docking site (Y1349/Y1365) of c-Met, as well as phosphorylation of AKT (S473) and ERK1/2 (T202/Y204), without affecting c-Met activation loop (Y1234/35) phosphorylation in GTL-16 cells. MK-2461 displays potent antiproliferative activity against a variety of tumor cell lines with IC50 of 0.1-30 μM. Orally administered MK-2461 inhibits c-Met phosphorylation in vivo, and tumor growth of GTL-16 xenografts, as well as the growth of NIH3T3 tumors harboring murine equivalents of human c-Met Y1230H and M1250T mutants.
| Cell Experiment | |
|---|---|
| Cell lines | SW480, HT29, SW620, Colo 205, HCT116, HCT15, Colo 201, SCC-9, H1993, H1048, GTL-16, SNU15, et al. |
| Preparation method | Exposing cells to various concentrations of MK-2461 for 72 hours. Using the ViaLight PLUS kit to mearsure the viability of tumor cells . |
| Concentrations | Dissolved in DMSO, final concentrations ~100 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Female nude CD-1 nu/nu mice inoculated s.c. with GTL-16 cells or c-Met mutant-transformed NIH3T3 cells |
| Formulation | Dissolved in DMSO, and diluted in saline |
| Dosages | ~134 mg/kg |
| Administration | Orally once or twice daily |
| Molecular Weight | 495.55 |
| Formula | C24H25N5O5S |
| CAS Number | 917879-39-1 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related c-Met Products |
|---|
| AMG-208
AMG-208 is a potent small molecular inhibitor c-Met with an IC50 of 9.3 nM. AMG-208 is also a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity. |
| BMS-777607
BMS-777607 is a selective and potent small-molecule met kinase inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively. |
| BMS 794833
BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor. |
| AMG-458
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively. |
| XL-184
Cabozantinib (XL184, BMS-907351) is a small molecule inhibits multiple receptor tyrosine kinases, specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM for VEGFR2 and Met respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
