ML327 is a blocker of MYC, which mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition. ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand. ML327 blocks the expression of MYC family of oncogenic transcription factors in all tested neuroblastoma cell lines. ML327 reduces SW620inv cell invasion through Matrigel by ~60% and reduces H520 cell invasion by ~30% in these in vitro assays.
In vivo, ML327 treatment significantly reduces tumor volume by three-fold over the two-week treatment period (p=0.02). Tumor explant weights are approximately three-fold smaller in the ML327-treated mice (p=0.01). Mice treated with ML327 lost 12% more body weight than vehicle treated mice.
| Molecular Weight | 366.37 |
| Formula | C19H18N4O4 |
| CAS Number | 1883510-31-3 |
| Solubility (25°C) | DMSO: ≥ 21 mg/mL (Need warming) |
| 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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MDEG-541 is a potent MYC-MAX degrader. |
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