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C188-9
別名：TTI 101
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.
CAS No. 432001-19-9
文献中Selleckの製品使用例（51）
製品安全説明書
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純度：
99.98%
99.98
C188-9関連製品
シグナル伝達経路
STAT阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| UM-SCC-17B | Cell growth assay | 0/0.1/0.3/1/3/10/100 μM | 36 h | IC50=0.7 ± 0.6 μM | 27027445 |
| SCC-61 | Cell growth assay | 0/0.1/0.3/1/3/10/100 μM | 36 h | IC50=14.8 ±2.9 μM | 27027445 |
| SCC-35 | Cell growth assay | 0/0.1/0.3/1/3/10/100 μM | 36 h | IC50=10.8 ± 0.0 μM | 27027445 |
| HN30 | Cell growth assay | 0/0.1/0.3/1/3/10/100 μM | 36 h | IC50=4.4 ± 0.1 μM | 27027445 |
| SK-N-DZ | Function assay | 10 μM | 28684419 | ||
| Y79 | Function assay | 10 μM | 28684419 | ||
| HepG2 | Cell viability assay | 48 h | IC50=10.19 μM | 28533225 | |
| PLC/PRF/5 | Cell viability assay | 48 h | IC50=11.83 μM | 28533225 | |
| Huh7 | Cell viability assay | 48 h | IC50=11.27 μM | 28533225 | |
| A549 | Function assay | 2.5 h | decreased pSTAT3 levels in a concentration-dependent manner starting at concentrations as low as 3 nM | 26410177 | |
| Kasumi-1 | Function assay | IC50=4.5 μM | 21447830 | ||
| THP-1 | Function assay | IC50=4.8 μM | 21447830 | ||
| GDM-1 | Function assay | IC50=5.0 μM | 21447830 | ||
| NB-1 | Function assay | IC50=8.3 μM | 21447830 | ||
| HL-60 | Function assay | IC50=5.3 μM | 21447830 | ||
| KG-1 | Function assay | IC50=4.1 μM | 21447830 | ||
| K562 | Apoptosis assay | induction of apoptosis with an EC50 of 43.6 μM | 21447830 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
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. | ||
|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| 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]. | |||
|---|---|---|---|---|
| 細胞実験 | 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. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-STAT3 / STAT3 / CEBPδ / Myostatin / p-Akt / Akt |
|
24011072 | |
| Immunofluorescence | VE-cadherin / β-catenin non-phosphorylated β-Catenin |
|
26948077 | |
| In Vivo | ||
| 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]. | |
|---|---|---|
| 動物実験 | 動物モデル | CD2F1 female mice received isogenic C26 tumor cell via s.c injection |
| 投与量 | 12.5 mg/kg | |
| 投与経路 | i.p. | |
化学情報
| 分子量 | 471.52 | 化学式 | C27H21NO5S |
| CAS No. | 432001-19-9 | SDF | Download C188-9 SDFをダウンロードする |
| Smiles | COC1=CC=C(C=C1)S(=O)(=O)NC2=CC(=C(C3=CC=CC=C32)O)C4=C(C=CC5=CC=CC=C54)O | ||
| 保管 | |||
|
In vitro |
DMSO : 94 mg/mL ( (199.35 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 2 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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