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).
| Molecular Weight | 462.97 |
| Formula | C26H27ClN4O2 |
| CAS Number | 1130067-06-9 |
| Solubility (25°C) | DMSO: ≥ 20 mg/mL Ethanol: ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
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Melittin is a PLA2 activator that stimulates the activity of low molecular weight PLA2 without increasing the activity of high molecular weight PLA2. |
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| SYN-020
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| IIAEK
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