GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2.
|Solubility (25°C)||DMSO 10 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Marzia Di Donato, et al. Targeting the Nerve Growth Factor Signaling Impairs the Proliferative and Migratory Phenotype of Triple-Negative Breast Cancer Cells
 Aditi A Bapat, et al. Blocking Nerve Growth Factor Signaling Reduces the Neural Invasion Potential of Pancreatic Cancer Cells
 Surabhi Shukla, et al. Mechanism for neurotropic action of vorinostat, a pan histone deacetylase inhibitor
 Tada-aki Kudo, et al. Induction of neurite outgrowth in PC12 cells treated with temperature-controlled repeated thermal stimulation
 Eun Joo Jung, et al. Proteomic analysis of novel targets associated with TrkA-mediated tyrosine phosphorylation signaling pathways in SK-N-MC neuroblastoma cells
|Related Trk Products|
Bedinvetmab (ZTS-00508841) is a canine monoclonal antibody (mAb) targeting nerve growth factor (NGF). Bedinvetmab inhibits NGF interaction with tropomyosin receptor kinase A (trkA) and p75 neurotrophin receptor (p75NTR) receptors. Bedinvetmab can be used for the research of osteoarthritis pain in dogs.
|MRTX849 ethoxypropanoic acid
LC-2 is a potent, first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50, between 0.25 and 0.76 μM).
Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
|Cyclotraxin B acetate
Cyclotraxin B acetate, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF.
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
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