5.08053

Mcl-1 Inhibitor II

• 同義詞: 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
• 經驗公式（希爾表示法）: C₂₃H₂₄F₃N₃O
• CAS號碼: 315698-17-0
• 分子量：: 415.45
• MDL號碼: MFCD02330695
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥95% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 25 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: FC(F)(F)c1ccc(cc1)C(N4CCN(CC4)CC)c2c(c3ncccc3cc2)O
• InChI 密鑰: NGAPBLRRJSKIRT-UHFFFAOYSA-N

描述

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
Mcl-1

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

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

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable