| Identification | Back Directory | [Name]
MT477 | [CAS]
328069-91-6 | [Synonyms]
MT477
tetramethyl 6'-[(2,5-dioxopyrrolidin-1-yl)acetyl]-7'-methoxy-5',5'-dimethyl-5',6'-dihydrospiro[1,3-dithiole-2,1'-thiopyrano[2,3-c]quinoline]-2',3',4,5-tetracarboxylate | [Molecular Formula]
C31H30N2O12S3 | [MDL Number]
MFCD01068171 | [MOL File]
328069-91-6.mol | [Molecular Weight]
718.77 |
| Hazard Information | Back Directory | [Description]
MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays. | [Uses]
MT477 is a potent protein kinase C (PKC) inhibitor. MT477 induces apoptosis and necrosis. MT477 decreases the protein expression of Ras-GTP, p-Erk1/2, p-Elk1. MT477 shows antitumor activity[1]. | [in vivo]
MT477 (33, 100, 1000 μg/kg; i.p.; once a day on days 1, 4, 8, 16, 18, 20) shows antitumor activity[1]. | Animal Model: | 6-week-old male nude mice (A431 cells) [1] | | Dosage: | 33, 100, 1000 μg/kg | | Administration: | I.p.; once a day on days 1, 4, 8, 16, 18, 20 | | Result: | Significant decreased in tumor volume of 24.5% by the third week at 1 mg/kg. |
| Animal Model: | 6-week-old male nude mice (H226 cells) [1] | | Dosage: | 1 mg/kg | | Administration: | I.p.; once a day on days 1, 4, 8, 20, 24, 28 | | Result: | Inhibited tumor growth by 43.6% and observed no weight loss. |
| [References]
[1] Jasinski P, et al. A novel quinoline, MT477: suppresses cell signaling through Ras molecular pathway, inhibits PKC activity, and demonstrates in vivo anti-tumor activity against human carcinoma cell lines. Invest New Drugs. 2008 Jun;26(3):223-32. DOI:10.1007/s10637-007-9096-x |
|
| Company Name: |
PHARMEKS Ltd.
|
| Tel: |
+7 (495) 702-9648 |
| Website: |
www.pharmeks.com |
|