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Tamnorzatinib

CAS No. : 1646839-59-9

MCE 站：Tamnorzatinib

产品活性：Tamnorzatinib (ONO-7475) 是一种有效的、选择性的、具有口服活性的 Axl/Mer 抑制剂，IC₅₀ 值分别为 0.7 nM 和 1.0 nM。Tamnorzatinib 使 AXL 过表达的 EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感，抑制耐药细胞的产生和耐药性的维持。Tamnorzatinib 联合 Osimertinib (HY-15772) 为 EGFR 突变非小细胞肺癌 (NSCLC) 的研究提供了一个光明的前景。

研究领域：Protein Tyrosine Kinase/RTK  |  Neuronal Signaling

作用靶点：TAM Receptor  |  Trk Receptor

In Vitro: Tamnorzatinib is against recombinant human AXL with IC₅₀ values of 0.414 nM ａnd 0.7 nM in off-chip MSA ａnd ACD cell-based tyrosine kinase assay, respectively. It is against AXL, MER, TYRO3, TRKB, PDGFR alpha, TRKA, ａnd FLT3 activities with IC₅₀ values of 0.7 nM, 1.0 nM, 8.7 nM, 15.8 nM, 28.9 nM, 35.7 nM ａnd 147 nM, respectively in a Cell-based Tyrosine Kinase assay.
Tamnorzatinib (0.0001 μM-1 μM; 72 hours) increases the sensitivity to Osimertinib ａnd Dacomitinib ａnd reduces the viability of high AXL-expressing PC-9 ａnd HCC4011 cells, but not of low-AXL-expressing HCC827 cells. Besides, Tamnorzatinib enhances Osimertinib efficacy on the viability of cell lines PC-9, PC-9KGR, ａnd HCC4011, ａnd H1975, all of which express high levels of AXL. But it has a marginal effect on the viability of cell lines HCC827, HCC4006, ａnd H3255 with low levels of AXL.
Tamnorzatinib (1 μM; 4 or 48 hours) combines with Osimertinib markedly inhibits the phosphorylation of AXL, AKT, ａnd p70S6K compared with the treatment of the high-AXL-expressing cell lines treated with Osimertinib alone at 4 hours. It combines with osimertinib increases cleaved PARP in PC-9 ａnd HCC4011 cells compared with the treatment with Osimertinib alone.

In Vivo: Tamnorzatinib (oral gavage; 10 mg/kg or combines with 5 mg/kg Osimertinib; 29 days) treatment alone has little effect on the tumor growth. Besides, Osimertinib alone causes tumor regression within one week, but the tumors reappear within three weeks. The combined initial treatment causes tumor regression ａnd the size of tumors is maintained for 4 weeks. No apparent adverse events, including weight loss are observed during these treatments.

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