MT477

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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406119

CAS#: 328069-91-6

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.

Price and Availability

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Pricing updated 2020-06-01. Prices are subject to change without notice.

MT477 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406119
Name: MT477
CAS#: 328069-91-6
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

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

Technical Data

Appearance:

Solid powder

Purity:

>98%

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

Additional Information

References

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.

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