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
• 実験式（ヒル表記法）: C₂₃H₂₄F₃N₃O
• CAS番号: 315698-17-0
• 分子量: 415.45
• MDL番号: MFCD02330695
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥95% (HPLC)
• 品質水準: 100
• フォーム: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 25 mg/mL
• 保管温度: 2-8°C
• SMILES記法: FC(F)(F)c1ccc(cc1)C(N4CCN(CC4)CC)c2c(c3ncccc3cc2)O
• InChI Key: NGAPBLRRJSKIRT-UHFFFAOYSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Mcl-1

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable