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508053 Mcl-1 Inhibitor II - CAS 315698-17-0 - Calbiochem

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Sinónimos: Myeloid Cell Leukemia-1 Inhibitor II, 7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol

Primary Target: Mcl-1
508053
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Descripción

Tabla espec. clave

CAS #Empirical Formula
315698-17-0C₂₃H₂₄F₃N₃O

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Número de referenciaEmbalaje Cant./Env.
5080530001 Frasco de vidrio 10 mg
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Description
OverviewA cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM142-161 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 t1/2 values of 40 min and 55 min, respectively.
Catalogue Number508053
Brand Family Calbiochem®
SynonymsMyeloid Cell Leukemia-1 Inhibitor II, 7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol
References
ReferencesRichard, D.J., et al. 2013. Bioorg. Med. Chem. 21, 6642.
Product Information
CAS number315698-17-0
FormWhite powder
Hill FormulaC₂₃H₂₄F₃N₃O
Chemical formulaC₂₃H₂₄F₃N₃O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary TargetMcl-1
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze(-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Número de referencia GTIN
5080530001 04055977242812