Synonym
MT477; MT 477; MT-477
IUPAC/Chemical Name
tetramethyl 6'-(2-(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
InChi Key
AQFSTZWCFIWEMA-UHFFFAOYSA-N
InChi Code
InChI=1S/C31H30N2O12S3/c1-30(2)25-19(14-9-8-10-15(41-3)21(14)33(30)18(36)13-32-16(34)11-12-17(32)35)31(20(26(37)42-4)22(46-25)27(38)43-5)47-23(28(39)44-6)24(48-31)29(40)45-7/h8-10H,11-13H2,1-7H3
SMILES Code
O=C(C1=C(C(OC)=O)SC2=C(C31SC(C(OC)=O)=C(C(OC)=O)S3)C4=C(N(C(CN5C(CCC5=O)=O)=O)C2(C)C)C(OC)=CC=C4)OC
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>5 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
718.77
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Ouelaa-Benslama R, De Wever O, Hendrix A, Sabbah M, Lambein K, Land D, Prévost G, Bracke M, Hung MC, Larsen AK, Emami S, Gespach C. Identification of a GαGβγ, AKT and PKCα signalome associated with invasive growth in two genetic models of human breast cancer cell epithelial-to-mesenchymal transition. Int J Oncol. 2012 Jul;41(1):189-200. doi: 10.3892/ijo.2012.1457. Epub 2012 Apr 30. PubMed PMID: 22552300.
2: Jasinski P, Zwolak P, Terai K, Vogel RI, Borja-Cacho D, Dudek AZ. MT477 acts in tumor cells as an AURKA inhibitor and strongly induces NRF-2 signaling. Anticancer Res. 2011 Apr;31(4):1181-7. PubMed PMID: 21508363.
3: Jasinski P, Zwolak P, Terai K, Borja-Cacho D, Dudek AZ. PKC-alpha inhibitor MT477 slows tumor growth with minimal toxicity in in vivo model of non-Ras-mutated cancer via induction of apoptosis. Invest New Drugs. 2011 Feb;29(1):33-40. doi: 10.1007/s10637-009-9330-9. Epub 2009 Oct 1. PubMed PMID: 19795097.
4: Jasinski P, Zwolak P, Terai K, Dudek AZ. Novel Ras pathway inhibitor induces apoptosis and growth inhibition of K-ras-mutated cancer cells in vitro and in vivo. Transl Res. 2008 Nov;152(5):203-12. doi: 10.1016/j.trsl.2008.09.001. Epub 2008 Oct 11. PubMed PMID: 19010291.
5: Jasinski P, Welsh B, Galvez J, Land D, Zwolak P, Ghandi L, Terai K, Dudek AZ. 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. Epub 2007 Oct 24. PubMed PMID: 17957339.
