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Synonyms | TTI 101 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H21NO5S |
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分子量 | 471.52 | CAS No. | 432001-19-9 | |
Solubility (25°C)* | 体外 | DMSO | 94 mg/mL (199.35 mM) | |
Ethanol | 3 mg/mL (6.36 mM) | |||
Water | 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. |
製品説明 | C188-9 (TTI 101) is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. |
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in vitro | C188-9 is a small-molecule inhibitor of Stat3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases[1]. |
in vivo | Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors[2]. |
細胞アッセイ | 細胞株 | HNSCC cell line, UM-SCC-17B |
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濃度 | 0, 0.1, 0.3, 1, 3, 10, 30 μM | |
反応時間 | 24 h | |
実験の流れ | UM-SCC-17B cells were incubated with various doses (0/0.1/0.3/1/3/10/30μM) of C188 or C188-9 for 24 hrs. |
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動物実験 | 動物モデル | CD2F1 female mice received isogenic C26 tumor cell via s.c injection |
投薬量 | 12.5 mg/kg | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Cells, 2018, 7(8)]
Targeting FLT3-TAZ signaling to suppress drug resistance in blast phase chronic myeloid leukemia [ Mol Cancer, 2023, 10.1186/s12943-023-01837-4] | PubMed: 37932786 |
FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(24):e2302613] | PubMed: 37345586 |
Transcriptional and chromatin profiling of human blood innate lymphoid cell subsets sheds light on HIV-1 pathogenesis [ EMBO J, 2023, e114153.] | PubMed: 37382276 |
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25] | PubMed: 36670508 |
JAK-STAT Signaling in Inflammatory Breast Cancer Enables Chemotherapy-Resistant Cell States [ Cancer Res, 2023, 83(2):264-284] | PubMed: 36409824 |
Hedgehog receptors exert immune-surveillance roles in the epidermis across species [ Cell Rep, 2023, 42(8):112929] | PubMed: 37527037 |
Honokiol prevents chronic cerebral hypoperfusion induced astrocyte A1 polarization to alleviate neurotoxicity by targeting SIRT3-STAT3 axis [ Free Radic Biol Med, 2023, 202:62-75] | PubMed: 36997099 |
CRISPR/Cas9-engineering of HMC-1.2 cells renders a human mast cell line with a single D816V-KIT mutation: An improved preclinical model for research on mastocytosis [ Front Immunol, 2023, 14:1078958] | PubMed: 37025992 |
Guizhi Fuling capsule relieves memory deficits by inhibition of microglial neuroinflammation through blocking JAK2/STAT3 pathway in presenilin1/2 conditional double knockout mice [ Front Immunol, 2023, 14:1185570] | PubMed: 37465679 |
Adenosine receptor A2b confers ovarian cancer survival and PARP inhibitor resistance through IL-6-STAT3 signalling [ J Cell Mol Med, 2023, 10.1111/jcmm.17802] | PubMed: 37278400 |
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。