iCRT14

製品コードS8704 バッチS870401

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₁H₁₇N₃O₂S
	分子量	375.44	CAS No.	677331-12-3
Solubility (25°C)*	体外	DMSO	37 mg/mL (98.55 mM)
		Water	Insoluble
		Ethanol	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	iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.
in vitro	iCRT14 suppresses the transcriptional activity of canonical Wnt signaling, downregulates Wnt/β-catenin-induced target genes, and inhibits the growth of colorectal cancer cells in vitro^[1]. iCRT14 shows a modest reduction in the amount of Dvl but has no effect on Dvl phosphorylation itself. iCRT14 inhibits the Wnt responsive STF16-luc reporter in mammalian HEK293 cells with an IC50 of 40.3 nM. iCRT14 can also interfere with TCF binding to DNA in addition to its ability to influence TCF-β-catenin interaction^[2].
in vivo	Administration of iCRT14 to the HCT116 and HT29 xenograft models reveals a marked decrease in CycD1, coincided with reduced proliferation of the tumors. Furthermore, these effects are correlated with a marked reduction (∼50%) in the initial growth rate of tumors within the first 3 wk (∼day 19) of compound administration. After day 19, however, the rate of tumor growth is comparable with that of DMSO-treated control. Throughout the course of the study, the mice does not display any signs of systemic toxicity or weight loss that would indicate off-target or nonspecific effects. The compound may be metabolized rapidly in vivo, thus reducing its bioavailability^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Rat2 cells
	濃度	25 and 50 μM
	反応時間	2 h
	実験の流れ	Rat2 cells are pretreated with iCRTs at the indicated doses and stimulated for 2 h with Wnt3a or Wnt5a. Cell lysate is harvested for western analysis of Dvl2 phosphorylation.
動物実験	動物モデル	HCT116 and HT29 xenograft models (implanted tumor cells in athymic nude mice)
	投薬量	50 mg/kg
	投与方法	i.p.

参考

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：

Upregulation of β-catenin signaling represents a single common pathway leading to the various phenotypes of spinal degeneration and pain [ Bone Res, 2023, 11(1):18]	PubMed: 37059724
Regulation of the WNT-CTNNB1 signaling pathway by severe fever with thrombocytopenia syndrome virus in a cap-snatching manner [ mBio, 2023, e0168823.]	PubMed: 37882780
β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354]	PubMed: 35255110
Cytoplasmic SHMT2 drives the progression and metastasis of colorectal cancer by inhibiting β-catenin degradation [ Theranostics, 2021, 11(6):2966-2986]	PubMed: 33456583

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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