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.
|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: ≥ 21 mg/mL (Need warming)|
Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma.
Rellinger EJ, et al. Oncotarget. 2017 Jul 20;8(53):91040-91051. PMID: 29207623.
ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand.
Rellinger EJ, et al. Biochem Biophys Res Commun. 2017 Sep 16;491(2):463-468. PMID: 28716733.
Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.
An H, et al. Oncotarget. 2015 Sep 8;6(26):22934-48. PMID: 26082441.
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