Trk Receptor Inhibitor

Trk-IN-11 (Compound 14h) is a potent inhibitor of TRK (IC₅₀ = 1.4, 1.8 nM, against TrkA, TrkA^G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-11 has the potential for the research of cancer disease.

TrkA-IN-10 (PI-15R) is a TrkA inhibitor with the IC₅₀ values of 17 nM, 8 nM, and 5 nM for TrkA, TrkB and TrkC, respectively. TrkA-IN-10 can be used in cancer research.

TRK-IN-13 is a potent inhibitor of TRK. Protein kinases play a critical role in the control of cell growth and differentiation and are responsible for the control of a wide variety of cellular signal transduction processes. TRK-IN-13 has the potential for the research of TRK-related diseases (extracted from patent WO2012034091A1, compound X-24).

(R)-Larotrectinib is a potent TRK inhibitor with an IC₅₀ value of 28.5 nM for TrkA. (R)-Larotrectinib can be used for researching cancer, inflammatory and certain infectious diseases

Compound cpd-1 is a small molecule Trks inhibitor with good antitumor activity.

MEDI-1912 is a human monoclonal antibody (mAb) targeting NGF/bNGF. MEDI-1912 inhibits signaling through TrkA and p75 receptors. MEDI-1912 can be used in chronic pain research.

YTB53 is a MNK1 and MNK2 inhibitor with IC₅₀s of 37 nM and 9 nM, respectively. YTB53 inhibits PDGFRα, TRKB and FLT3 in leukemia cells. YTB53 induces cell cycle arrest, apoptosis, pyroptosis, and mitochondrial dysfunction. YTB53 exhibits antiangiogenic effects. YTB53 can be used for the study of acute myeloid leukemia (AML).

TRK-IN-22 (compound 11) is a TRK inhibitor. TRK-IN-22 (compound 11), a typical type I inhibitor, covers the ATP-binding pocket of TRKA.

Trk-IN-1 (example 9), a potent tropomyosin-related kinase (Trk) inhibitor, shows potency against TrkA (3.7 nM) and TrkB (94 nM), respectively.

Anti-TrkB/NTRK2 Antibody is a human antibody expressed in CHO cells, targeting TrkB. Anti-TrkB/NTRK2 Antibody can be referenced as Human IgG2 kappa, Isotype Control (HY-P99002).

TrkA-IN-7 (Compound 4) is an inhibitor of Tropomyosin Receptor Kinase A (TrkA) with a K_d value of 40 μM.

Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC₅₀ = 0.86, 6.92 nM, against TrkA, TrkA^G595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-10 (IC₅₀ = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity.

TRK II-IN-1 is a potent type II TRK inhibitor, with IC₅₀s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKA^G667C, respectively. TRK II-IN-1 also inhibits FLT3, RET, and VEGFR2 with IC₅₀s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers.

JND4135 is a Type II TRK inhibitor with IC₅₀ values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model.

Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC₅₀ = 0.2-0.7 nM).

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC₅₀ values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.

(R,S)-Selitrectinib ((R,S)-LOXO-195) (compound 17) is a Trk inhibitor with activity against cancers harboring Trk inhibitor-resistant point mutations in NTRK1, NTRK2, or NTRK3 genes. (R,S)-Selitrectinib can be used for the research of trk inhibitor-resistant cancer.

Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC₅₀ values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA^G595R, TrkA^G667C, TrkA^G667S, TrkA^F589L and TrkC^G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis.

Larotrectinib-d₄ (LOXO-101-d₄) is the deuterium labeled Larotrectinib (HY-12866). Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

TRK-IN-27 (Compound 14q) is a potent TRK inhibitor with good kinase selectivity. TRK-IN-27 effectively inhibits tumor growth.