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Merck

5.08053

Mcl-1 Inhibitor II

Synonym(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

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About This Item

Empirical Formula (Hill Notation):
C23H24F3N3O
CAS Number:
315698-17-0
Molecular Weight:
415.45
MDL number:
MFCD02330695
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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InChI key

NGAPBLRRJSKIRT-UHFFFAOYSA-N

SMILES string

FC(F)(F)c1ccc(cc1)C(N4CCN(CC4)CC)c2c(c3ncccc3cc2)O

assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 25 mg/mL

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Mcl-1
Reversible: yes

Disclaimer

Toxicity: Standard Handling (A)

General description

A 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.

Other Notes

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

Packaging

Packaged under inert gas

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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