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Trk-IN-20

CAS No. : 2460924-63-2

MCE 站：Trk-IN-20

产品活性：Trk-IN-20 是一种 3- 乙烯基咪唑衍生物，是 Trk 抑制剂。Trk-IN-20 通过抑制磷酸化来抑制 Trk 激酶功能，抑制 TrkA/B/C 的 IC₅₀s 分别为 1.6 nM、2.9 nM 和 2.0 nM。

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

作用靶点：Trk Receptor

In Vitro: NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers.
Trk-IN-20 (compound 7mb) (0.031, or 0.018 μM, respectively; 72 h) exhibits strong inhibition against the Larotrectinib-resistant cells with NTRK1-G667C or NTRK3-G696A mutations with IC₅₀s of 0.031 ａnd 0.018 μM, respectively.
Trk-IN-20 (compound 7mb) (9-22 nM; 72 h) inhibits BaF3 murine cells stably transformed with NTRK oncogenic fusions including CD74-NTRK1, ETV6-NTRK2 ａnd ETV6-NTRK3 with IC₅₀s of 15, 22, ａnd 9 nM, respectively.
Trk-IN-20 (compound 7mb) (0.32, 1.6, 8, 40, 200; 6 h) inhibits activation of Trk ａnd its downstream proteins in BaF3-CD74-NTRK1, BaF3-ETV6-NTRK2, BaF3-ETV6-NTRK3 cells.
Trk-IN-20 (compound 7mb) tightly bound to ATP-binding site of TrkA, TrkB, ａnd TrkC with binding constant (K_d) values of 1.6, 3.1 ａnd 4.9 nM, respectively.

In Vivo: Trk-IN-20 (compound 7mb) (p.o.; 10 mg/kg) shows short half-life of 1.39 hours ａnd a low oral bioavailability of 8.79% in rats.

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