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Tamnorzatinib
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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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Neuronal Signaling Compound Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Orally Active Compound Library | Anti-Lung Cancer Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | DS-1205b free base | (3aR)-Selitrectinib | LM22B-10 | TRK-IN-16 | ANA-12 | UNC2250 | PF-06733804 | Larotrectinib sulfate | Trk-IN-10 | AZ-23 | GNF-8625 monopyridin-N-piperazine hydrochloride | Axl-IN-5 | Trk-IN-7 | TRK-IN-23 | Protein kinase inhibitor 5 | TrkB-IN-1 | UNC4203 | Axl-IN-3 | Bedinvetmab | TrkA-IN-1 | PF-6683324 | UNC569 | Cabozantinib | Cyclotraxin B | PF-06737007 | Bemcentinib | Axl-IN-12 | TRK-IN-21 | Sacibertinib
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