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Taletrectinib

CAS No. : 1505515-69-4

MCE 国际站：Taletrectinib

产品活性：Taletrectinib (DS-6051b) 是一种有效的口服活性下一代选择性 ROS1/NTRK 抑制剂。Taletrectinib 分别以 0.207、0.622、2.28 和 0.98 nM 的 IC₅₀ 对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用。Taletrectinib 还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：ROS Kinase

In Vitro: The IC₅₀ of Taletrectinib (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM.
Taletrectinib (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro.
Taletrectinib potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells.
Taletrectinib partially suppresses phospho-NTRK1 at 10 nM, and completely suppresses by 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP-competitive manner. Taletrectinib almost completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but did not inhibit other 152 kinases strongly.
Taletrectinib effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation.

In Vivo: Taletrectinib (DS-6051b) (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity.
Taletrectinib (6.25-200 mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells.
Taletrectinib (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor 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  |  Targeted Diversity Library  |  Mitochondrial Protection Compound Library  |  Membrane Protein-targeted Compound Library  |  Highly Selective Inhibitors Library  |  ALK/ROS1-IN-1  |  MitoPQ  |  GGTI-2418  |  Iruplinalkib  |  Antitumor agent-60  |  Taletrectinib free base  |  Anticancer agent 59  |  AChE/BChE/BACE-1-IN-2  |  Antitumor agent-55  |  ROS kinases-IN-2  |  GGTI-2154  |  Antibacterial agent 69  |  AChE/BChE/BACE-1-IN-1  |  Antibacterial agent 110  |  Phyltetralin  |  Entrectinib  |  AChE/BChE-IN-9  |  10-Methyl-9-(phenoxycarbonyl)acridinium (fluorosulfonate)  |  Anticancer agent 58  |  Capsanthin  |  Salvigenin  |  Pinealon  |  Antibacterial agent 70  |  Zidesamtinib  |  Anticancer agent 76  |  F-1  |  Lamalbid  |  Mefloquine  |  Merestinib  |  Lorlatinib

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