VU-0155069 is a potent and selective phospholipase D1 (PLD1) inhibitor with IC50 values of 46 and 933 nM for PLD1 and PLD2, respectively. VU0155069 inhibits migration of human and mouse breast cancer cell lines in transwell assays. VU0155069 significantly decreases invasive migration in breast cancer cell lines (MDA-231, 4T1 and PMT).
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 20 mg/mL
Ethanol: ≥ 20 mg/mL
PEA-15 potentiates H-Ras-mediated epithelial cell transformation through phospholipase D.
Sulzmaier FJ, et al. Oncogene. 2012 Jul 26;31(30):3547-60. PMID: 22105357.
Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
Scott SA, et al. Nat Chem Biol. 2009 Feb;5(2):108-17. PMID: 19136975.
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