SKL2001 is a novel agonist of Wnt/β-catenin pathway with anti-cancer activity. SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex. SKL2001 inhibited proliferation of colon cancer cells cultured in 3D spheroid and induced them accumulation in the G0/G1 phase of the cell cycle with a reduced c-myc level. SKL2001 (5, 10, and 30 μM) stabilizes intracellular β-catenin in 3T3-L1 cells. SKL2001 (40 μM) significantly inhibits the proliferation of HCT116 spheroids independently of cytotoxicity and the inhibition is reversible.
|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.
|Solubility||DMSO ≥ 60 mg/mL|
Role of Wnt/β-catenin pathway agonist SKL2001 in Caerulein-induced acute pancreatitis.
Huang HL, et al. Can J Physiol Pharmacol. 2019 Jan;97(1):15-22. PMID: 30326193.
SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex.
Ohashi W, et al. Biochem Biophys Res Commun. 2017 Nov 25;493(3):1342-1348. PMID: 28970068.
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