C188-9 (TTI-101)

製品コードS8605 バッチS860503

印刷

化学情報

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

180 mg/mL (381.74 mM)

Ethanol

2 mg/mL (4.24 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.700mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 94 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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. This compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/25787076/
https://pubmed.ncbi.nlm.nih.gov/27027445/

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：

Adipocyte CLDN5 promotes thermogenesis and energy expenditure through regulation of IL10 expression [ Nat Commun, 2025, 16(1):6151]	PubMed: 40610440
Immunoreceptor CD300a regulates ischemic tissue damage and adverse remodeling in the mouse heart and kidney [ J Clin Invest, 2025, 135(19)e184984]	PubMed: 40705472
EGFR-STAT3 activation provides a therapeutic rationale for targeting aggressive ETV1-positive prostate cancer [ Mol Oncol, 2025, 10.1002/1878-0261.70069]	PubMed: 40808640
Morphological regulation of wound repair astrocytes by leucine zipper-bearing kinase-AKT signaling after spinal cord injury [ Exp Neurol, 2025, 393:115379]	PubMed: 40680877
Involvement of STAT3 activation in ameliorating all-trans-retinal-induced ferroptosis in photoreceptor-derived 661W cells in vitro [ Exp Eye Res, 2025, 253:110280]	PubMed: 39947311
Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis [ Sci Adv, 2025, 11(4):eadq2395]	PubMed: 39841821
HLF transactivates TFEB to promote gallbladder cancer stem cells' self-renewal and determines tumor response to distinct therapies [ Sci Adv, 2025, 11(32):eadv6723]	PubMed: 40779629
Macrophage biomimetic nanoparticle-targeted functional extracellular vesicle micro-RNAs revealed via multiomics analysis alleviate sepsis-induced acute lung injury [ J Nanobiotechnology, 2024, 22(1):362]	PubMed: 38910259
IL-27 disturbs lipid metabolism and restrains mitochondrial activity to inhibit γδ T17 cell-mediated skin inflammation [ Cell Death Dis, 2024, 15(7):491]	PubMed: 38982043
Induction of SUSD2 by STAT3 Activation Is Associated with Tumor Recurrence in HER2-Positive Breast Cancer [ Cells, 2024, 14(1)19]	PubMed: 39791720

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。