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Catalog No.
Product Name
Application
Product Information
Citations
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TRK, ROS1, ALK inhibitor
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.- Angelina T Regua, .et al. , Cancer Lett, 2024, Jun 7:597:217023 PMID: 38852701
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IGF-1R inhibitor
BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
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TRK inhibitor
GNF-5837 is a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.- Tanimizu N, .et al. , Development, 2018, Apr 25;145(9). pii: dev159095 PMID: 29615468
- Shargh VH, .et al. , Nanomedicine (Lond), 2017, May;12(9):977-989 PMID: 28440712
- Shargh VH, .et al. , Int J Pharm, 2016, Dec 30;515(1-2):527-534 PMID: 27793712
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Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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HER2 inhibitor
Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. -
CDK Inhibitor
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity. -
Multiple Kinase Inhibitor
KRC-108 is a potent aminopyridine that functions as a multiple kinase inhibitor, targeting c-Met and its variants, Ron, Flt3, and TrkA with IC50 values ranging from 3 nM to 80 nM. It demonstrates significant biological activity by inducing cell cycle arrest, promoting apoptotic cell death, and facilitating autophagy. KRC-108 showcases robust anti-tumor effects in vivo, particularly in HT29 colorectal cancer and NCI-H441 lung cancer xenograft models using athymic BALB/c nu/nu mice, making it a valuable reagent for cancer research applications. -
SERT/NET Inhibitor
Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity. -
TrkA/Akt Inhibitor
HS-345 is a selective inhibitor of the TrkA/Akt signaling pathway, demonstrating significant anti-cancer effects in pancreatic cancer models. It inhibits the growth and proliferation of pancreatic cancer cells while inducing apoptosis. Moreover, HS-345 disrupts angiogenesis by downregulating the expression of HIF-1α and VEGF. This compound shows potential as a valuable tool for research into pancreatic cancer therapies. -
Trk Inhibitor
Sacibertinib is a selective tyrosine kinase inhibitor targeting Trk receptors, demonstrating an EC50 of 110 nM for EGFR-TK phosphorylation and 244 nM for HER2. It exhibits pronounced antineoplastic activity, making it a valuable tool in cancer research. Sacibertinib is suitable for studies focused on kinase signaling pathways and potential therapeutic interventions in tumors associated with Trk activation. -
TRAF6-p62 Inhibitor
TRAF6 peptide is a selective inhibitor of the TRAF6-p62 interaction. It effectively disrupts the ubiquitination of TrkA in NGF-dependent signaling pathways. This peptide demonstrates significant potential for research in neurological disorders, including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, epilepsy, and stroke. -
CDK2 Inhibitor
TrkA Inhibitor is a selective CDK2 inhibitor, demonstrating an IC50 of 0.69 μM against CDK1. This compound is particularly valuable in research focused on chemotherapy-induced alopecia, allowing for the investigation of mechanisms involved in hair follicle cycling and potential therapeutic interventions. Its specificity for CDK2 makes it a useful tool in examining cell cycle regulation and associated pathways in various biological contexts. -
Aurora A/B Kinase inhibitor
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1. -
multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
CSF-1R inhibitor
TE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis. -
TRK inhibitor
Larotrectinib (LOXO-101, ARRY-470) is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC.
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TRK inhibitor
LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. -
RTK inhibitor
Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth. -
pan-Trk inhibitor
PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively. -
ALK/TRKA/TRKB/TRKC inhibitor
Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7?nM for wild-type recombinant ALK kinase. -
ROS1/TRK inhibitor
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. -
TKI inhibitor
Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor (TKI), with IC50s of 0.6 nM, <2.5 nM for TRKA and TRKC respectively. -
TRK Inhibitor
TRK II-IN-1 is a selective type II TRK inhibitor, exhibiting IC50 values of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the TRKAG667C mutant, respectively. Additionally, it demonstrates inhibitory activity against FLT3, RET, and VEGFR2 with IC50 values of 1.3, 9.9, and 71.1 nM, respectively. This compound is valuable for research into TRK-driven cancers and related signaling pathways. -
PLK4 Inhibitor
CZS-241 is a selective Polo-like Kinase 4 (PLK4) inhibitor, exhibiting an IC50 of 2.6 nM. In addition to its primary activity, CZS-241 also inhibits TRKA with an IC50 of 2.74 μM. This compound induces apoptosis and effectively arrests the cell cycle at the S/G2 phase. CZS-241 demonstrates potent antiproliferative effects against leukemia cell lines while maintaining safety profiles in normal cell lines, making it a valuable tool for cancer research. -
TRK Inhibitor
JND4135 is a Type II TRK inhibitor that effectively targets TRKA, TRKB, and TRKC with IC50 values of 2.79, 3.19, and 3.01 nM, respectively. This compound is capable of overcoming resistance associated with TRK xDFG and other mutant forms, inhibiting the phosphorylation of both wild-type and mutant TRKs, as well as their downstream signaling pathways. JND4135 induces G0/G1 phase cell cycle arrest and apoptosis in BaF3–CD74-TRKA-G667C cells and exhibits potent antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model, highlighting its potential for cancer research and therapy. -
Multikinase Inhibitor
Multi-kinase-IN-6 is a potent multikinase inhibitor targeting TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It demonstrates significant antiproliferative effects in cancer cell lines, with IC50 values of 3.36 μM for MCF7, 1.40 μM for HCT116, and 3.49 μM for EKVX. Furthermore, Multi-kinase-IN-6 induces cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells while promoting apoptosis, making it a valuable tool for cancer research and therapeutic studies. -
Pan-Trk Inhibitor
Pan-Trk-IN-3 is a potent pan-Trk inhibitor that effectively targets TrkA, TrkB, and TrkC, along with various drug-resistant mutants, exhibiting IC50 values as low as 2 nM. This compound demonstrates significant antitumor activity and induces apoptosis in cancer cells. Pan-Trk-IN-3 is suitable for research applications focusing on cancer biology and therapeutic development aimed at overcoming Trk-related resistance mechanisms. -
TrkB Inhibitor
PC-046 is a potent multitarget inhibitor of tyrosine receptor kinase B (TrkB), IRAK-4, and Pim-1, with IC50 values of 13.4 μM, 15.4 μM, and 19.1 μM, respectively. This compound demonstrates significant cytotoxicity against BxPC3 pancreatic cancer cells, with an IC50 range of 7.5-130 nM. PC-046 effectively induces apoptosis and disrupts the cell cycle at the G2/M phase in these cells. Additionally, it showcases promising antitumor efficacy and favorable pharmacokinetic properties in murine models, making it a valuable tool for cancer research. -
TRK Inhibitor
IHMT-TRK-284 is a potent, orally active inhibitor targeting TRK kinases, exhibiting IC50 values of 10.5 nM, 0.7 nM, and 2.6 nM against TRKA, TRKB, and TRKC, respectively. This compound demonstrates a favorable selectivity profile within the kinome and shows promising in vivo efficacy in antitumor models. IHMT-TRK-284 is valuable for studies investigating the role of TRK signaling in various cancers and for the development of targeted therapeutic strategies. -
TRK Inhibitor
TRK-IN-32 is a potent inhibitor of TRK proteins, effectively targeting TRKWT, TRKG595R, and TRKG667C with IC50 values of 0.08 nM, 2.14 nM, and 0.68 nM, respectively. This compound exhibits significant antiproliferative activity against Ba/F3 cell lines expressing various TRK fusion proteins, including wild type and mutant forms. TRK-IN-32 also induces apoptosis in Ba/F3-TRKAWT and Ba/F3-TRKAG667C cells, making it a valuable tool for investigating the role of TRK signaling in a range of cancers, including thyroid cancer and secretory breast carcinoma. -
TRK Inhibitor
TRK-IN-23 is a selective TRK inhibitor demonstrating potent biological activity with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKAG595R, TRKAF589L, and TRKAG667C, respectively. This compound effectively induces apoptosis in Ba/F3 cells expressing TRKAG595R and TRKAG667C. TRK-IN-23 is valuable for researchers investigating TRK signaling pathways and potential therapeutic interventions in TRK-driven malignancies. -
TrkB Inhibitor
Cyclotraxin B is a selective inhibitor of the TrkB receptor, effectively crossing the blood-brain barrier. It inhibits brain-derived neurotrophic factor (BDNF) induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B exhibits notable analgesic and anxiolytic properties, making it a valuable tool for research into neurological disorders and pain management. -
TrkA Inhibitor
TrkA-IN-3 is a potent allosteric inhibitor of TrkA, exhibiting an IC50 of 22.4 nM. It demonstrates over 8000-fold selectivity for TrkA compared to TrkB and TrkC, making it a valuable tool for targeted studies. This compound is applicable in pain research, aiding in the exploration of neurogenic pain mechanisms and potential therapeutic interventions. -
Trk Receptor Inhibitor
GNF-8625 monopyridin-N-piperazine hydrochloride is a potent inhibitor of the Tropomyosin receptor kinase (Trk) family. This compound effectively disrupts the signaling pathways associated with Trk receptors, which are implicated in neurotrophic signaling and oncogenesis. GNF-8625 is utilized in research applications focused on neurobiology, cancer pharmacology, and targeted therapies to elucidate the role of Trk signaling in tumor growth and nerve regeneration. -
Trk Inhibitor
Utatrectinib (AZD-7451) is a selective and potent oral inhibitor of tropomyosin receptor kinases (Trk). By inhibiting TrkC activation, Utatrectinib effectively disrupts tumorigenic signaling pathways associated with various cancers. This compound is primarily utilized in research focused on neurotrophin receptor modulation and its implications in oncogenesis. -
Tyrosine Kinase Inhibitor
Paltimatrectinib is a potent tyrosine kinase inhibitor with an IC50 of less than 10 nM for tropomyosin receptor kinases A (TrkA). This compound demonstrates significant biological activity in inhibiting cell proliferation and migration associated with cancer and inflammatory diseases. Paltimatrectinib is applicable in research focused on therapeutic strategies for malignancies and inflammatory disorders. -
TrkA Inhibitor
TrkA-IN-4 is a potent allosteric inhibitor of TrkA, functioning as a proagent of TrkA-IN-3 with an IC50 value of 22.4 nM. This compound demonstrates significant antinociceptive effects, making it an important tool for research in pain modulation and neurobiology. Its orally active formulation enhances its utility in pharmacological studies exploring the role of TrkA in various pain-related pathways. -
Trk Receptor Inhibitor
TrkA-IN-1 is a selective inhibitor of the Tropomyosin-related kinase A (TrkA) receptor, demonstrating an IC50 of 99 nM in cell-based assays. This compound exhibits analgesic activity, making it valuable in research focused on pain pathways and neurobiology. TrkA-IN-1 can be utilized to explore the role of TrkA in various biological processes and disease models related to pain and neurodegeneration. -
Trk Inhibitor
LPM4870108 is a potent pan-Trk inhibitor, targeting wild-type and mutant variants with IC50 values of 0.2 nM for TrkC, 2.4 nM for TrkA, 3.5 nM for TrkAG595R, and 2.3 nM for TrkAG667C. It demonstrates selectivity for Trk over ALK, with an IC50 of 182 nM. LPM4870108 exhibits significant anti-tumor activity, making it a valuable tool for studying Trk-related oncogenic signaling pathways and developing targeted cancer therapies. -
TRKA/C Inhibitor
TRK-IN-24 is a potent inhibitor of Trk receptors, specifically targeting TRKA, TRKC, TRKAG595R, TRKAG667C, and TRKAF589L, with IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM, respectively. This compound demonstrates significant antitumor activity in xenograft models, including BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C. Additionally, TRK-IN-24 effectively inhibits the proliferation of Ba/F3 cells harboring various single mutants, achieving IC50 values ranging from 1.43 to 47.56 nM. This makes TRK-IN-24 a valuable tool for research applications focused on targeted cancer therapies. -
TRK Inhibitor
Trk-IN-7 is a potent TRK inhibitor targeting TRKA, TRKB, and TRKC, with IC50 values ranging from 0.25 to 10 nM. Additionally, Trk-IN-7 demonstrates significant inhibitory activity against EML4-ALK and various ALK mutations, including G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A, with IC50 values ranging from 5 to 50 nM. This compound is valuable for research in neurotrophic signaling and cancer biology, particularly involving TRK and ALK pathways. -
TRK Inhibitor
Trk-IN-8 is a potent TRK inhibitor that exhibits IC50 values of 0.42 nM for TRKAa, 0.89 nM for TRKA(G595R), and 1.5 nM for TRKC(G623R). This compound is effective in selectively targeting Tropomyosin receptor kinase (TRK) signaling pathways, making it a valuable tool for research in cancer biology and therapeutic development. Its high selectivity and potency facilitate studies of TRK-related oncogenic processes and potential treatment strategies for TRK fusion-positive tumors.
