5.08321

Dihydroorotate Dehydrogenase Inhibitor, Brequinar

• Synonyme(s) : Dihydroorotate Dehydrogenase Inhibitor, Brequinar, 6-fluoro-2-(2ʹ-fluoro-1,1ʹ-biphenyl-4-yl)-3-methyl-4-quinoline-carboxylic acid sodium salt, NSC 368390, DuP 785, NSC 368390, DuP 785, 6-fluoro-2-(2ʹ-fluoro-1,1ʹ-biphenyl-4-yl)-3-methyl-4-quinoline-carboxylic acid sodium salt
• Formule empirique (notation de Hill): C₂₃H₁₄F₂NNaO₂
• Numéro CAS: 96201-88-6
• Poids moléculaire : 397.35
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 12 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C
• InChI: 1S/C23H15F2NO2.Na/c1-13-21(23(27)28)18-12-16(24)10-11-20(18)26-22(13)15-8-6-14(7-9-15)17-4-2-3-5-19(17)25;/h2-12H,1H3,(H,27,28);/q;+1/p-1
• Clé InChI: PZOHOALJQOFNTB-UHFFFAOYSA-M

Description

Description générale

A quinolinecarboxylic acid derivative with immunosuppressive and anti-neoplastic properties. Inhibits pyrimidine synthesis by blocking the activity of mammalian mitochondrial dihydroorotate dehydrogenase (DHODH; IC₅₀ = 12 nM). Does not affect DHODH in non-mammalian species. Also reported to inhibit glycosylation of adhesion molecules. Potentiates the sensitivity of U1690 small cell lung cancer cells to TRAIL-induced apoptosis and synergistically enhances the anti-tumor effects of doxorubicin ( ~100 µM).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
DHODH

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

He, T. et al. 2013. Oncogene32, in press.
Hurt, D.E., et al. 2006. Bioorg. Med. Chem. Lett.16, 1610.
Schnellrath, L. et al. 2011. Int. J. Antimicrob. Agents.38, 435.
Batt, D.G., et al. 1995. Bioorg. Med. Chem. Lett.14, 1549.
Allison, A., et al. 1993. Transplantation Proc.25, 67.
Cramer, D. et al. 1992. Transplantation.53, 303.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable