Napabucasin (BBI608)

製品コードS7977 バッチS797702

印刷

化学情報

Chemical Structure Synonyms BBI608 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C14H8O4
分子量 240.21 CAS No. 83280-65-3
Solubility (25°C)* 体外 DMSO 14 mg/mL (58.28 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.
in vitro Napabucasin downregulates stemness gene expression driven by Stat3 and cancer stemness properties, and effectively inhibits self-renewal of stemness-high cancer cells with IC50 ranged from 0.291~1.19 μM, on inhibition on normal stem cells. [1]
in vivo In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis. [1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Cancer stem cells U87-MG, U118, COLO205, DLD1, SW480, HCT116, FaDu, ACHN, SNU-475, Huh7, HepG2, H1975, A549, H460, CAOV-3, SW-626, PaCa2.
濃度 ~2 μM
反応時間 72 h
実験の流れ

For cancer stem cells, spheres are dissociated and plated under cancer stem cell culture conditions on coated 96-well plates. After 72 h of culture, wells are dosed with the indicated compounds. Seventy-two hours or 24 h after dosing, CellTiter-Glo 2.0 is added to each well, and the luminescence is measured as described by the manufacturer. IC50 values are calculated by fitting a four parameter dose–response curve to normalized data using GraphPad Prism software. For bulk cells, cells are plated at 5,000 cells per well on 96-well plates. Twenty-four hours after plating, cells are treated with the indicated compounds. Viability is determined at 72 h as described above.
動物実験 動物モデル Mice bearing PaCa-2 xenografts
投薬量 20 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Serum amyloid A promotes glycolysis of neutrophils during PD-1 blockade resistance in hepatocellular carcinoma [ Nat Commun, 2024, 15(1):1754] PubMed: 38409200
ADAR1-mediated RNA editing of SCD1 drives drug resistance and self-renewal in gastric cancer [ Nat Commun, 2023, 14(1):2861] PubMed: 37208334
Targeting VCP potentiates immune checkpoint therapy for colorectal cancer [ Cell Rep, 2023, 42(11):113318] PubMed: 37865914
Alcohol reshapes a liver premetastatic niche for cancer by extra- and intrahepatic crosstalk-mediated immune evasion [ Mol Ther, 2023, 31(9):2662-2680] PubMed: 37469143
CRISPRi screens in human iPSC-derived astrocytes elucidate regulators of distinct inflammatory reactive states [ Nat Neurosci, 2022, 25(11):1528-1542] PubMed: 36303069
Ligand-mediated PAI-1 inhibition in a mouse model of peritoneal carcinomatosis [ Cell Rep Med, 2022, 3(2):100526] PubMed: 35243423
Targeted inhibition of STAT3 induces immunogenic cell death of hepatocellular carcinoma cells via glycolysis [ Mol Oncol, 2022, 16(15):2861-2880] PubMed: 35665592
Identification of Novel Therapeutic Targets for Fibrolamellar Carcinoma Using Patient Derived Xenografts and Direct from Patient Screening [ Cancer Discov, 2021, candisc.0872.2020] PubMed: 34127480
Exploring transcriptional regulators Ref-1 and STAT3 as therapeutic targets in malignant peripheral nerve sheath tumours [ Br J Cancer, 2021, 10.1038/s41416-021-01270-8] PubMed: 33658640
Targeting EphA2 suppresses hepatocellular carcinoma initiation and progression by dual inhibition of JAK1/STAT3 and AKT signaling [ Cell Rep, 2021, 34(8):108765] PubMed: 33626345

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。