C188-9

製品コードS8605 バッチS860504

印刷

化学情報

 Chemical Structure Synonyms TTI 101 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C27H21NO5S

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.

溶剤液(一定の濃度)を調合する

生物活性

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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HNSCC cell line, UM-SCC-17B
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.

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.

カスタマーフィードバック

Data from [Data independently produced by , , Cells, 2018, 7(8)]

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:

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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。

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