Trk Receptor Inhibitor

TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK^G595R IC₅₀ = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC₅₀ = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC₅₀ = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line.

TRK-IN-34 is an orally active TRKand TRKC mutant kinase inhibitor, with IC₅₀ values of 0.75 nM and 0.96 nM against TRKA^G595R and TRKA^G667C, respectively. TRK-IN-34 inhibits the kinase activities of TRKA^G595R and TRKA^G667C at the functional level. TRK-IN-34 inhibits the proliferation of TRKA-transfected cells, exerts tumor growth-inhibitory effects and achieves partial tumor regression in xenograft models. TRK-IN-34 can be used to study TRK inhibitor-resistant cancers driven by the TRKA^G667C mutation.

NPA101.3 is an orally active RET receptor tyrosine kinase and VEGFR2 inhibitor (RET IC₅₀ = 0.001 μM, RET^V804M IC₅₀ = 0.008 μM, VEGFR2 IC₅₀ = 0.003 μM). NPA101.3 inhibits purified TRKA (IC₅₀ = 32 nM) and CSF1R (IC₅₀ = 46 nM). NPA101.3 completely suppresses tumor formation in RET^/C634Y-transformed cells and also attenuates tumor formation in HRAS^/G12V-transformed cells. NPA101.3 can be used in the research of RET-driven cancers.

CRB-0089 is a human monoclonal antibody (mAb) targeting NGF/bNGF. CRB-0089 can be used in analgesia research.

Antitumor agent-223 is an anticancer agent and TRK inhibitor. Antitumor agent-223 exerts potent antitumor activity against liver cancer and breast cancer. Antitumor agent-223 can be used for the research of hepatocellular carcinoma and breast cancer.

TrkC-IN-1 (Compound 6c) is an inhibitor of TrkC. The IC₅₀ values for EBC-1 and HT-29 cells are 3.3-7.1 and 7.3-10.2 μΜ, respectively. TrkC-IN-1 is expected to be used in the research of the anti-cancer field.

TRK-IN-18 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2021148805A1, compound 7).

PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC₅₀ of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC₅₀ of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice.

Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA^G667C and ETV6-TRKC^G696C fusion proteins with IC₅₀s of 6 nM and 1.7 nM, respectively. Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC₅₀ values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.

TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA^G667C degradation (DC₅₀ = 24.69 nM; D_max > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1^G667C cells with an IC₅₀ value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research.

Anizatrectinib (hTrkA-IN-1) is an orally active and blood-brain barrier-penetrant TrkA kinase/hERG channel inhibitor. Anizatrectinib can be used for research on TrkA-mediated related diseases, such as pain, cancer, inflammation, and inflammatory diseases.

NMS-P626 is an inhibitor of TRKA, TRKB, and TRKC, with IC₅₀ values of 8 nM, 7 nM, and 3 nM, respectively. NMS-P626 inhibits the growth of KM12 cells by suppressing the phosphorylation of TPM3-TRKA and downstream signaling in KM12 cells, with an IC₅₀ of 19 nM for KM12 cells. NMS-P626 can be used in colorectal cancer research.

2-Bromo-6-methoxynaphthalene (Standard) is the analytical standard of 2-Bromo-6-methoxynaphthalene. This product is intended for research and analytical applications. 2-Bromo-6-methoxynaphthalene is an active intermediate in the production of anti-inflammatory agents like Naproxen and Nabumetone by Heck reaction. 2-Bromo-6-methoxynaphthalene has potential anti-inflammatory properties and Tyrosine-protein inhibitor properties. 2-Bromo-6-methoxynaphthalene can be used for the research of cancer.

Utatrectinib (Standard) is the analytical standard of Utatrectinib (HY-102066). This product is intended for research and analytical applications. Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.

TRK-IN-25 (compound 16) is a Trk inhibitor with antiproliferative activity against cancer cells. TRK-IN-25 can be used in cancer research.

Wrightiadione is a selective natural tetracyclic isoflavone kinase inhibitor with inhibitory activity against TrkA and PLK3. The IC₅₀ values of Wrightiadione against TrkA and PLK3 are 55.8 μM and 9.0 μM, respectively. Wrightiadione is found in the dried bark of Wrightia tomentosa. Wrightiadione can be used in studies of leukemia, kinase inhibition and cancer-related signaling pathways.

(3aR)-Selitrectinib ((3aR)-LOXO-195) is an isform of Selitrectinib (HY-101977), which is a next-generation TRK kinase inhibitor, with IC₅₀s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.

ONO-7579 is an orally active TRKA inhibitor that suppresses tumor growth by inhibiting the phosphorylation of TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research.