ONT-093, also known as OC-144-093, is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy. ONT-093 could inhibit P-gp and reverse multidrug resistance at nM concentrations with no effect on paclitaxel pharmacokinetics. OC144-093 is the least non-specifically toxic Pgp inhibitor described to date, with an average cytostatic IC50 of >60 microM in 15 cell types. OC144-093 may represent an ideal candidate for use in enhancement of AED blood-brain barrier penetration.
Chemical Formula: C32H38N4O
Exact Mass: 494.30456
Molecular Weight: 494.67
Elemental Analysis: C, 77.70; H, 7.74; N, 11.33; O, 3.23
Chemical Name: (E)-4,4'-(2-(4-(3-ethoxyprop-1-en-1-yl)phenyl)-1H-imidazole-4,5-diyl)bis(N-isopropylaniline)
InChi Code: InChI=1S/C32H38N4O/c1-6-37-21-7-8-24-9-11-27(12-10-24)32-35-30(25-13-17-28(18-14-25)33-22(2)3)31(36-32)26-15-19-29(20-16-26)34-23(4)5/h7-20,22-23,33-34H,6,21H2,1-5H3,(H,35,36)/b8-7+
Appearance: Light yellow to orange
Purity: >98% (or refer to the Certificate of Analysis)
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
Zhang N, Zhang Z, Wong IL, Wan S, Chow LM, Jiang T. 4,5-Di-substituted benzyl-imidazol-2-substituted amines as the structure template for the design and synthesis of reversal agents against P-gp-mediated multidrug resistance breast cancer cells. Eur J Med Chem. 2014 Aug 18;83:74-83. doi: 10.1016/j.ejmech.2014.06.016. Epub 2014 Jun 10. PubMed PMID: 24952376.
Modok S, Mellor HR, Callaghan R. Modulation of multidrug resistance efflux pump activity to overcome chemoresistance in cancer. Curr Opin Pharmacol. 2006 Aug;6(4):350-4. Epub 2006 May 11. Review. PubMed PMID: 16690355.
Vaalburg W, Hendrikse NH, Elsinga PH, Bart J, van Waarde A. P-glycoprotein activity and biological response. Toxicol Appl Pharmacol. 2005 Sep 1;207(2 Suppl):257-60. Review. PubMed PMID: 16043202.
Chi KN, Chia SK, Dixon R, Newman MJ, Wacher VJ, Sikic B, Gelmon KA. A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5. PubMed PMID: 16012790.
Ross DD. Modulation of drug resistance transporters as a strategy for treating myelodysplastic syndrome. Best Pract Res Clin Haematol. 2004 Dec;17(4):641-51. Review. PubMed PMID: 15494300.
Kuppens IE, Bosch TM, van Maanen MJ, Rosing H, Fitzpatrick A, Beijnen JH, Schellens JH. Oral bioavailability of docetaxel in combination with OC144-093 (ONT-093). Cancer Chemother Pharmacol. 2005 Jan;55(1):72-8. Epub 2004 Aug 17. PubMed PMID: 15316750.
Products are for research use only. Not for human use.
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