| DC10631 |
PF-06273340
|
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. |
| DC77199 |
VMD-928
|
VMD-928 is an orally active, allosteric, irreversible and selective tropomyosin receptor kinase A (TrkA) inhibitor. VMD-928 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. VMD-928 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma. |
| DC77198 |
BNN27
|
BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable. |
| DC74435 |
PTX-BD10-2
|
PTX-BD10-2 (BD10-2) is a selective, brain-penetrant small molecule TrkB/C receptor partial agonist, shows survival-promoting activity. |
| DC74434 |
Emzeltrectinib
|
Emzeltrectinib is a potent, selective neurotrophic factor tyrosine kinase receptor TrkB inhibitor, shows potential for treatment of Trk kinase-mediated tumor. |
| DC74433 |
Anizatrectinib
|
Anizatrectinib is a potent and orally active inhibitor of TrkA kinase with potential for inflammatory disease such as prostatitis. |
| DC71253 |
IHMT-TRK-284
|
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. |
| DC71183 |
TIY-7
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model. |
| DC71141 |
D5261
|
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor. |
| DC70879 |
Utatrectinib
|
Utatrectinib (AZD7451, AZ12607092) is a potent, selective, small molecule pan-Trk (NTRK) inhibitor with IC50 of 0.2-3.0 nM against TrkA, TrkB, and TrkC.Binding of AZD7451 to TrkA, TrkB, and TrkC would be expected to inhibit responses associated with NGF, BDNF, and NT3, respectively.AZD7451 completely blocked TrkC activation and associated tumorigenic behaviors at sub-micromolar concentrations in normal salivary gland tissue.AZD7451 showed efficacy and low toxicity in pre-clinical studies on adenoid cystic carcinoma (ACC) tumors engrafted in mice.AZD7451 potently inhibited in vitro growth and proliferation of the KM12 cell line harboring the NTRK1-fusion at 2 nM, AZD7451 inhibited proliferation of H460 cells at 5 nM, with TRKA phosphorylation inhibition. |
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