Trk-IN-20 

Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC₅₀ values of 1.6 nM, 2.9 nM and 2.0 nM, respectively^[1].

NTRK1 is a proto-oncogene in colon cancer, Trk inhibitors have been detected to against a variety of human cancers^[1].
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^[1].
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^[1].
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^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

376.40

C₂₂H₁₈F₂N₄

2460924-63-2

FC1=CC([C@@H](C)NC2=CC3=C(C=C2)NN=C3/C=C/C4=NC=CC=C4)=CC(F)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Duan Y, et al. Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors. Eur J Med Chem. 2020 Oct 1. 203:112552.  [Content Brief]