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Taletrectinib

CAS No. : 1505515-69-4

MCE 站：Taletrectinib

产品活性：Taletrectinib (DS-6051b) 是一种有效的口服活性新一代选择性 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 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

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：Crizotinib  |  Lorlatinib  |  Entrectinib  |  Repotrectinib  |  Merestinib  |  Tempo  |  ALK/ROS1-IN-1  |  F-1  |  Taletrectinib free base  |  WY-135

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