5.08053
Mcl-1 Inhibitor II
別名:
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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この商品について
実験式（ヒル表記法）:
C23H24F3N3O
CAS番号:
分子量:
415.45
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥95% (HPLC)
Quality Segment
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
SMILES string
FC(F)(F)c1ccc(cc1)C(N4CCN(CC4)CC)c2c(c3ncccc3cc2)O
InChI key
NGAPBLRRJSKIRT-UHFFFAOYSA-N
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Mcl-1
Mcl-1
Reversible: yes
Packaging
Packaged under inert gas
Other Notes
Richard, D.J., et al. 2013. Bioorg. Med. Chem.21, 6642.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。