CA3 (CIL56)

製品コードS8661 バッチS866102

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₃H₂₇N₃O₅S₂

分子量

489.61

CAS No.

300802-28-2

Solubility (25°C)*

体外

DMSO

98 mg/mL (200.15 mM)

Water

Insoluble

Ethanol

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。	0.500mg/ml (1.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 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 it; 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	CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).
in vitro	CA3 (CIL56) strongly inhibits esophageal adenocarcinoma cell growth in vitro. It can effectively suppress tumor cell proliferation, induce apoptosis, reduce tumor sphere formation, and the population of ALDH1+ cells. This compound specially inhibits Tead/YAP1 transcriptional activity but shows no inhibitory activity on other transcriptional factors-Super-TOP/Wnt, CBF1/Notch, and AP-1 after cotransfection of their respective individual promoter luciferases in 293T cells. It preferentially inhibits CSC properties enriched in radiation-resistant esophageal adenocarcinoma cells^[1].
in vivo	CA3 (CIL56) exerts strong antitumor activity in xenograft model with no apparent toxicity^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SKGT-4 and JHESO cells
	濃度	0.5 and 1 μmol/L
	反応時間	48 hours
	実験の流れ	SKGT-4 and JHESO cells are seeded onto 6-well plates (1 × 10⁵/well) in DMEM and cultured for 24 hours to allow for cell attachment. The cells are then treated with 0.1% DMSO (control) or CA3 (CIL56) at different doses as indicated for 48 hours. Next, the cells are harvested, fixed with methanol, washed, treated with RNase A, and stained for DNA with propidium iodide, and their DNA histograms and cell-cycle phase distributions are analyzed using flow cytometry.
動物実験	動物モデル	A JHESO xenograft model of esophageal adenocarcinoma
	投薬量	1 mg/kg/mouse
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/29167315/

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：

YAP as a therapeutic target to reverse trastuzumab resistance [ Gastric Cancer, 2025, 10.1007/s10120-025-01630-w]	PubMed: 40542295
Targeting Latent HIV Reservoirs: Effectiveness of Combination Therapy with HDAC and PARP Inhibitors [ Viruses, 2025, 17(3)400]	PubMed: 40143326
Blocking YAP1-Liprin-β2 interaction impedes metastasis and promotes tumor suppression in head and neck squamous carcinoma [ Sci Rep, 2025, 15(1):26968]	PubMed: 40707583
SHP1 and its downstream p38/SP1/PI3K/YAP/Notch-1 signaling in trophoblast cells suppressed the progression of Preeclampsia via inhibiting proliferation of SMCs [ Sci Rep, 2025, 15(1):16205]	PubMed: 40346122
GPRC5A promotes lung colonization of esophageal squamous cell carcinoma [ Nat Commun, 2024, 15(1):9950]	PubMed: 39550386
Hippo-signaling-controlled MHC class I antigen processing and presentation pathway potentiates antitumor immunity [ Cell Rep, 2024, 43(4):114003]	PubMed: 38527062
The Hippo pathway terminal effector TAZ/WWTR1 mediates oxaliplatin sensitivity in p53 proficient colon cancer cells [ BMC Cancer, 2024, 24(1):587]	PubMed: 38741073
The Hippo pathway terminal effector TAZ/WWTR1 mediates oxaliplatin sensitivity in p53 proficient colon cancer cells [ BMC Cancer, 2024, 24(1):587]	PubMed: 38741073
YAP-TEAD inhibition is associated with upregulation of an androgen receptor mediated transcription program providing therapeutic escape [ FEBS Open Bio, 2024, 10.1002/2211-5463.13901]	PubMed: 39300603
EDA Fibronectin Microarchitecture and YAP Translocation During Wound Closure [ bioRxiv, 2024, 2024.09.23.614581]	PubMed: 39386582

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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