JW 74 is a inhibitor of canonical Wnt signaling. JW 74 targets the β-catenin destruction complex (GSK-3 beta /AXIN/APC). JW 74 increases AXIN2 and decreases active β-catenin levels in colorectal cancer (CRC) cells. JW 74 also arrests cell cycle in G1 and inhibits proliferation of CRC cells in vitro. JW 74 inhibits tumor growth and formation in mouse models.
|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 45 mg/mL|
Apigen induces apoptosis through a mitochondria/caspase-pathway in human breast cancer MDA-MB-453 cells.
Choi, et al. J Clin Biochem Nutr. 2009;44: 260. PMID: 19430615.
|Related Wnt/beta-catenin Products|
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM.
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Adavivint (SM04690) is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter.
Gallocyanine is a small molecule DKK1 inhibitor, which blocks DKK1 inhibitory activity on Wnt signaling.
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