5.08053

Mcl-1 Inhibitor II

• Synonyme(s) : Mcl-1 Inhibitor II, 7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol, Myeloid Cell Leukemia-1 Inhibitor II, Myeloid Cell Leukemia-1 Inhibitor II, 7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol
• Formule empirique (notation de Hill): C₂₃H₂₄F₃N₃O
• Numéro CAS: 315698-17-0
• Poids moléculaire : 415.45
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥95% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 25 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM_142-161 for Mcl-1, but not Bcl-xL, binding (IC₅₀ = 310 nM vs >40 µM; [Mcl-1] & [Bcl-xL] = 6.25 nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC₅₀ = >10 µM). Antiproliferation potencies against 2 murine lymphoma cell lines (GI₅₀ = 300 nM/ MCl1-1780 & 1.1 µM/Bcl2-1863) and 11 human cancer lines of various origins (GI₅₀ from 1.6 to 25 µM) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment. Stability studies using murine and human liver microsome preparations reveal t_1/2 values of 40 min and 55 min, respectively.

A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM_142-161 for Mcl-1, but not Bcl-xL, binding (IC₅₀ = 310 nM vs >40 µM; [Mcl-1] & [Bcl-xL] = 6.25 nM). Antiproliferation potencies against 2 murine lymphoma cell lines and 11 human cancer lines of various origins (GI₅₀ from 0.3 to 25 µM) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Mcl-1

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

Richard, D.J., et al. 2013. Bioorg. Med. Chem.21, 6642.

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