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MedKoo product information:
ONT-093
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MedKoo Code#: 202055
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Name: ONT-093
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CAS#: 216227-54-2
Synonym:
Code name: OC144-093; OC-144-093; ONT-093. Chemical name:
**N-[4-[2-[4-[3-Ethoxy-1(E)-propenyl]phenyl]-4-[4-(isopropylamino)phenyl]-1H-imidazol-5-yl]phenyl]-N-isopropylamine;
**2-[4-[3-Ethoxy-1(E)-propenyl]phenyl]-4,5-bis[4-(isopropylamino)phenyl]-1H-imidazole
IUPAC/Chemical name:
(E)-4,4'-(2-(4-(3-ethoxyprop-1-en-1-yl)phenyl)-1H-imidazole-4,5-diyl)bis(N-isopropylaniline)
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Chemical structure
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Theoretical analysis
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Chemical Formula: C32H38N4O
Exact Mass: 494.30456
Molecular Weight: 494.67
m/z: 494.30456 (100.0%), 495.30792 (34.6%),
496.31127 (5.8%), 495.30160 (1.5%)
Elemental Analysis: C, 77.70; H, 7.74; N,
11.33; O, 3.23
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Availability and price:
ONT-093 (OC144-093), 98% (HPLC), is
available through custom synthesis
To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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ONT-093 (formerly OC-144-093) is a
P-glycoprotein pump inhibitor, for the potential reversal of multidrug
resistance in patients undergoing cancer chemotherapy. The compound was
also being evaluated for its potential enhancement of the oral
bioavailability of drugs that are P-glycoprotein substrates requiring
either high dosage forms or intravenous administration, and for the
potential improvement of central nervous system penetration of
P-glycoprotein substrate drugs [source: Prakash Mistry, Adrian Folkes.
ONT-093 (Ontogen). Current opinion in investigational drugs (London,
England : 2000). 2002 Nov;3(11): 1666-71 ]
A phase I pharmacokinetic study of
ONT-093: Doses of ONT-093 achieving serum concentrations
associated with biological activity were well tolerated in combination
with standard doses of paclitaxel. Toxicities of the combination in this
schedule were mainly attributable to paclitaxel and dose-limiting
toxicity was limited to febrile neutropenia. There was an apparent
pharmacokinetic interaction between paclitaxel and ONT-093, possibly
related in part to the excipient, Cremophor, present in the paclitaxel
formulation. [source: Invest New Drugs. 2005 Aug;23(4):311-5.]
Current developer:
Ontogen (Originator).
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
6: Thomas H, Coley HM. Overcoming multidrug resistance in cancer: an
update on the clinical strategy of inhibiting p-glycoprotein. Cancer
Control. 2003 Mar-Apr;10(2):159-65. Review. PubMed PMID: 12712010.
7: Mistry P, Folkes A. ONT-093 (Ontogen). Curr Opin Investig Drugs. 2002
Nov;3(11):1666-71. Review. PubMed PMID: 12476971.
8: Guns ES, Denyssevych T, Dixon R, Bally MB, Mayer L. Drug interaction
studies between paclitaxel (Taxol) and OC144-093--a new modulator of MDR
in cancer chemotherapy. Eur J Drug Metab Pharmacokinet. 2002
Apr-Jun;27(2):119-26. PubMed PMID: 12064370.
9: Newman MJ, Dixon R, Toyonaga B. OC144-093, a novel P glycoprotein
inhibitor for the enhancement of anti-epileptic therapy. Novartis Found
Symp. 2002;243:213-26; discussion 226-30, 231-5. Review. PubMed PMID:
11990779.
10: Guns ES, Bullock PL, Reimer ML, Dixon R, Bally M, Mayer LD.
Assessment of the involvement of CYP3A in the vitro metabolism of a new
modulator of MDR in cancer chemotherapy, OC144-193, by human liver
microsomes. Eur J Drug Metab Pharmacokinet. 2001 Oct-Dec;26(4):273-82.
PubMed PMID: 11808870.
11: Kim KH. 3D-QSAR analysis of 2,4,5- and 2,3,4,5-substituted
imidazoles as potent and nontoxic modulators of P-glycoprotein mediated
MDR. Bioorg Med Chem. 2001 Jun;9(6):1517-23. PubMed PMID: 11408170.
12: Newman MJ, Rodarte JC, Benbatoul KD, Romano SJ, Zhang C, Krane S,
Moran EJ, Uyeda RT, Dixon R, Guns ES, Mayer LD. Discovery and
characterization of OC144-093, a novel inhibitor of
P-glycoprotein-mediated multidrug resistance. Cancer Res. 2000 Jun
1;60(11):2964-72. PubMed PMID: 10850444.
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