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MGCD265 is an orally bioavailable, small molecule tyrosine kinase inhibitor of Met, VEGFR1, VEGFR2, VEGFR3, Ron, and Tie2 with IC50 of 1 nM, 3 nM, 3 nM, 4 nM, 2 nM and 7 nM, respectively. Dysregulation of Met signaling has been implicated in the initiation, progression and metastasis of human cancers. Met is overexpressed in non-small-cell lung cancer and its lack of staining in normal lung tissue makes it an attractive target. Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs. MGCD-265 has demonstrated a favorable safety profile and can be combined safely with other cancer therapeutics such as docetaxel and erlotinib. In preclinical studies, MGCD265 demonstrated nanomolar potency in enzyme and cellular assays and up to 100% of tumor growth inhibition in a broad range of xenograft models. Daily oral administration of MGCD265 was found to be well tolerated at doses of 24, 48 and 96 mg/m2.
| Molecular Weight | 517.6 |
| Formula | C26H20FN5O2S2 |
| CAS Number | 875337-44-3 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Belalcazar A, et al. Expert Rev Anticancer Ther. Targeting the Met pathway in lung cancer.
| 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. |
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