5.38776

FGFR4 Inhibitor, BLU9931

• 同義詞: FGFR4 Inhibitor, BLU9931, Fibroblast Growth Factor Receptor 4 Inhibitor, BLU9931
• 經驗公式（希爾表示法）: C₂₆H₂₂Cl₂N₄O₃
• 分子量：: 509.38
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: solid
• 效力: 3 nM IC₅₀
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: −20°C

描述

一般說明

A cell-permeable anilinoquinazoline derivative that acts as a highly potent, irreversible, paralog selective inhibitor of fibroblast growth factor receptor 4 kinase (FGFR4; IC₅₀ = 3 nM; k_inact/K_I = 0.6 x 10⁵ (mol/L) ^-1s^-1). Acts by forming a covalent bond with Cys552 within the ATP-binding pocket of FGFR4. Has minimal effect on FGFR1, 2, and 3 (IC₅₀ = 591 nM, 493 nM, and 150 nM respectively) and does not display any activity towards a panel of 455 other protein kinases. Suppresses FGFR4 signaling and phosphorylation of downstream components in MDA-MB-453 cells. Also shown to be a potent inhibitor of downstream signaling in Hep 3B hepatocellular carcinoma (HCC) cells expressing FGF19 and induces caspase 3 and 7 activity. Inhibits the growth of Hep 3B HCC xenografts in murine model (100 mg/kg, b.i.d; p.o. for 21 days). Displays desirable pharmacokinetic properties with moderate bioavailability (18%) and t_1/2 = 2.3 h (~ 10 mg/kg, p.o.).

生化／生理作用

Cell permeable: yes

Primary Target
FGFR4

Reversible: no

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Hagel, M., et al. 2015. Cancer Discov.5, 424.

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