Catalog No.
Product Name
Application
Product Information
Product Citation
-
HER2 inhibitor
Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. -
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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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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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. -
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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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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TRK inhibitor
LOXO-101 is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. -
TrkB agonist
7,8-Dihydroxyflavone, a selective tyrosine kinase receptor B (neurotrophic factor/tropomyosin-receptor-kinase B; TrkB) agonist, may be used to help identify and differentiate the physiological effects and cell signaling pathways mediated by TrkB activation, such as those involving neuroprotection, memory, vasorelaxation and hypertension. -
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. -
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. -
TrkB receptor activator
N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor. -
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. -
TrkA agonist
Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic. -
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.
