Bioactivity | Tepotinib (EMD-1214063) is a potent and highly selective c-Met inhibitor with an IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Antitumor effects[1]. | ||||||||||||
Invitro | Tepotinib (EMD 1214063) inhibits IRAK4, TrkA, Axl, IRAK1, Mer, and TrkA with IC50s of 615, 1017, 1566, 2037, 2272, and 5716 nM, respectively[1].Exposure of A549 cells to EMD 1214063 results in inhibition of HGF-induced c-Met phosphorylation, with an average IC50 of 6 nM[1].EMD 1214063 (0.01 nM-30 μM) inhibits tumor cell proliferation and migration in vitro[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tepotinib 相关抗体: Cell Viability Assay[1] Cell Line: | ||||||||||||
In Vivo | Tepotinib (EMD 1214063) induces tumor regression in xenograft models[1].Tepotinib inhibit in vivo c-Met phosphorylation[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
CAS | 1100598-32-0 | ||||||||||||
Formula | C29H28N6O2 | ||||||||||||
Molar Mass | 492.57 | ||||||||||||
Appearance | 固体 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Bladt F, et al. EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res, 2013, 19(11), 2941-2951. [2]. Zhan N, et al. The Effect of Selective c-MET Inhibitor on Hepatocellular Carcinoma in the MET-Active, β-Catenin-Mutated Mouse Model. Gene Expr. 2018 May 18;18(2):135-147. |