| 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. |
| DC80396 |
CDK12-IN-9
|
CDK12-IN-9 is a potent and selective CDK12 inhibitor with an IC50 of 2.2 nM. CDK12-IN-9 inhibits pSER2 (a downstream marker of CDK12/13 activity). CDK12-IN-9 can be used for the research of cancer. |
| DC80184 |
ALK-IN-35
|
ALK-IN-35 is a ALK degrader with an IC50 of 0.74 nM. ALK-IN-35 inhibits ALK kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the ALK binding pocket, promotes ALK to form a partially unfolded conformation, and induces proteasomal degradation of ALK. ALK-IN-35 inhibits cancer cell proliferation. ALK-IN-35 can be used in research related to non-small cell lung cancer. |
| DC78628 |
Eratrectinib
|
Eratrectinib (Example 1) is a Trk inhibitor. Eratrectinib can be studied in research for tropomyosin receptor kinase-related diseases and cancers. |
| DC78269 |
Type II TRK inhibitor 3
|
Type II TRK inhibitor 3 (Compound 18d) is a Type II TRK inhibitor with IC50 values of 0.82, 1.82, and 0.12 nM for TRKAWT/G595R/G667C, respectively. Type II TRK inhibitor 3 exhibits antitumor activity. |
| 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. |