WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406119
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.
MedKoo Cat#: 406119
Chemical Formula: C31H30N2O12S3
Exact Mass: 718.09609
Molecular Weight: 718.77
Elemental Analysis: C, 51.80; H, 4.21; N, 3.90; O, 26.71; S, 13.38
This product is not in stock, which may be available by custom synthesis.
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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
Appearance: Solid powder
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
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, PrÃ©vost 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.