| Bioactivity | Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects[1][2][3]. |
| Invitro | Tepotinib hydrochloride 抑制 IRAK4、TrkA、Axl、IRAK1、Mer 和 TrkA，IC50 分别为 615、1017、1566、2037、2272 和 5716 nM[1]。Tepotinib hydrochloride 抑制 A549 细胞中 HGF 诱导的 c-Met 磷酸化，平均 IC50 为 6 nM[1]。Tepotinib (0.01 nM-30 μM) hydrochloride 可在体外抑制肿瘤细胞增殖和迁移[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Tepotinib hydrochloride 相关抗体: |
| In Vivo | Tepotinib hydrochloride 在异种移植模型中诱导肿瘤消退并抑制体内 c-Met 磷酸化[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 1103508-80-0 |
| Formula | C29H28N6O2.xHCl |
| Molar Mass | 492.57 (free base) |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. [3]. A. Naing, et al. IS4-1 - A Phase I Dose-Escalation Study of emd 1214063, an Oral Selective CMET Inhibitor, in Patients with Advanced Solid Tumors. Annals of Oncology. Volume 23, Supplement 11, October 2012, Page xi21. |
Tepotinib hydrochloride
CAS: 1103508-80-0 F: C29H28N6O2.xHCl W: 492.57 (free base)
Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibi
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