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CAS No. : 1802220-02-5
MCE 国际站:Repotrectinib
产品活性:Repotrectinib (TPX-0005) 是一种有效的 ROS1 (IC50=0.07 nM) 和 TRK (对 TRKA/B/C 的 IC50=0.83/0.05/0.1 nM) 抑制剂。Repotrectinib 有效抑制 WT ALK (IC50=1.01 nM)。Repotrectinib 具有抗癌活性。
研究领域:Protein Tyrosine Kinase/RTK | Neuronal Signaling
作用靶点:ROS Kinase | Trk Receptor | Anaplastic lymphoma kinase (ALK)
In Vitro: Repotrectinib (TPX-0005) inhibits mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM). Repotrectinib also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (IC50=1.04, 1.66, 5.3, and 6.96 nM, respectively).
?Repotrectinib effectively overcomes this primary resistance (IC50=100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50=13 nM) and the SRC substrate paxillin (IC50=107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib.
In Vivo: Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts.
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 | Macrocyclic Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Anti-Lung Cancer Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | Mitochondrial Protection Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | DS-1205b free base | LM22B-10 | ALK/ROS1-IN-1 | TRK-IN-16 | MitoPQ | Ceritinib | KRCA-0008 | GGTI-2418 | ANA-12 | Iruplinalkib | Antitumor agent-60 | ALK-IN-22 | PF-06733804 | Taletrectinib free base | Larotrectinib sulfate | Anticancer agent 59 | Trk-IN-10 | AZ-23 | GNF-8625 monopyridin-N-piperazine hydrochloride | JH-VIII-157-02 | Trk-IN-7 | NVP-TAE 684 | Protein kinase inhibitor 5 | AChE/BChE/BACE-1-IN-2 | TrkB-IN-1 | Bedinvetmab | Antitumor agent-55 | TrkA-IN-1 | ROS kinases-IN-2
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货号: HY-103022
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