5.33851

Cancer Stemness Inhibitor, BBI608

• 别名: Cancer Stemness Inhibitor, BBI608, 2-Acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione, 2-Acetylnaphtho[2,3-b]furan-4,9-dione, Spherogenesis Blocker, BBI-608, Napabucasin
• 经验公式（希尔记法）: C₁₄H₈O₄
• CAS号: 83280-65-3
• 分子量: 240.21
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥97% (HPLC)
• 品質等級: 100
• 形狀: solid
• 效力: 142 nM IC₅₀
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: brown
• 溶解度: DMSO: 50 mg/mL
• 儲存溫度: 2-8°C
• InChI: 1S/C14H8O4/c1-7(15)11-6-10-12(16)8-4-2-3-5-9(8)13(17)14(10)18-11/h2-6H,1H3
• InChI 密鑰: DPHUWDIXHNQOSY-UHFFFAOYSA-N

说明

一般說明

A cell-permeable, bioactive, non-toxic naphthofurandione analog that blocks STAT3-driven gene transcription. Selectively diminishes gene expression and self-renewal in stemness high cancer cells. Shown to be more effective in stemness high cancer cell population (IC₅₀ = 142 nM) compared to regular cancer cells (IC₅₀ = 395 nM). Reduces spherogenesis in CD44 expressing cancer cells without affecting the colony formation in CD34⁺ hematopoietic stem cells. Effectively reduces the levels of Nanog, Axl, Sox-2, Klf4, survivin, c-Myc, Bmi-1, and β-catenin within a few hours following treatment. Displays broad spectrum activity against stemness high cancer cells from multiple tumors (IC₅₀ = 291, 432, 624, 479, 549, and 729 nM for CAOV-3, SW-626, PaCa2, SNU-475, H1975, and U87-MG, respectively). Suppresses the growth of PaCa-2 xenografts in murine models that exhibited relapse of tumor growth (20 mg/kg, i.p, q.d.) following the cessation of 41-day gemcitabine treatment. Also shown to block cancer relapse, and spleen and liver metastasis in the intrasplenic nude mouse model injected with HT29 colon cancer cells.

A cell-permeable, bioactive, non-toxic naphthofurandione analog that blocks STAT3-driven gene transcription. Selectively diminishes gene expression and self-renewal in stemness high cancer cells. Shown to be more effective in stemness high cancer cell population (IC₅₀ = 142 nM) compared to regular cancer cells (IC₅₀ = 395 nM). Reduces spherogenesis in CD44 expressing cancer cells without affecting the colony formation in CD34⁺ hematopoietic stem cells. Effectively reduces the levels of Nanog, Axl, Sox-2, Klf4, survivin, c-Myc, Bmi-1, and β-catenin within a few hours following treatment. Displays broad spectrum activity against stemness high cancer cells from multiple tumors (IC₅₀ = 291, 432, 624, 479, 549, and 729 nM for CAOV-3, SW-626, PaCa2, SNU-475, H1975, and U87-MG, respectively). Suppresses the growth of PaCa-2 xenografts in murine models that exhibited relapse of tumor growth (20 mg/kg, i.p, q.d.) following the cessation of 41-day gemcitabine treatment. Also shown to block cancer relapse, and spleen and liver metastasis in the intrasplenic nude mouse model injected with HT29 colon cancer cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生化／生理作用

Cell permeable: yes

Primary Target
STAT3

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

Li, Y., et al. 2015. Proc. Natl. Acad. Sci. USA112, 1839.

法律資訊

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

安全信息

• 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