5.33851

Cancer Stemness Inhibitor, BBI608

• 別名: 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
• 実験式（ヒル表記法）: C₁₄H₈O₄
• CAS番号: 83280-65-3
• 分子量: 240.21
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• 形状: solid
• 有効性: 142 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: brown
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 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 Key: DPHUWDIXHNQOSY-UHFFFAOYSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
STAT3

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

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