Guadecitabine (SGI-110)

別名：S-110

製品コード：S7013 純度：99.93%

Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.

CAS No. 929904-85-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 145500	国内在庫あり
5mg	JPY 130500	国内在庫あり
25mg	JPY 328500	国内在庫あり
100mg	JPY 748500	国内在庫あり

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文献中Selleckの製品使用例（7）

製品安全説明書

現在のバッチを見る： S701301 DMSO] 100 mg/mL] false] Water] 50 mg/mL] false] Ethanol] Insoluble] false 純度： 99.93%

99.93

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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

生物活性

製品説明

Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.

Targets

DNA methyltransferase ^[1]

In Vitro
In vitro	Guadecitabine (SGI-110) is a 5-aza-2′-deoxycytidine-containing demethylating dinucleotide, which works via a mechanism similar to that of 5-aza-CdR after incorporation of its aza-moiety into DNA. However, it is well protected from deamination by cytidine deaminase. This compound (1 μM) induces a significant decrease in the level of methylation in both T24 and HCT116 cells and is able to induce robust p16 expression. It (1 μM) causes depletion of extractable DNMT1 in cells and decreases the plating efficiency of T24 bladder carcinoma cells in a dose-dependent manner, with no colonies forming at 10 μM concentration, which is quite similar to 5-aza-CdR in T24 cells. ^[1] It also shows immunomodulatory activity in vitro. At 1 μM, it induces/up-regulates the expression of several cancer/testis antigens (CTA) (i.e., MAGE-A1, MAGE-A2, MAGE-A3, MAGE-A4, MAGE-A10, GAGE1-2, GAGE 1-6, NY-ESO-1, and SSX 1-5) in cancer cell lines (cutaneous melanoma, mesothelioma, renal cell carcinoma, and sarcoma cells), both at mRNA and at protein levels. This compound also up-regulates the expression of HLA class I antigens and of ICAM-1, resulting in improved recognition of cancer cells by gp100-specific CTL. ^[2]
細胞実験	細胞株	UMUC-3 cells
	濃度	2 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentrations of Guadecitabine (SGI-110).

In Vivo
In Vivo	Guadecitabine (SGI-110) is as effective as 5-Aza-CdR, but is better tolerated in mice. It (10 mg/kg) displays potent activity on inducing p16 expression, reducing DNA methylation at the p16 promoter region, and retarding tumor growth in human xenograft. This compound is effective by both i.p. and s.c. deliveries. ^[3]
動物実験	動物モデル	Human bladder cancers xenografts EJ6
	投与量	10 mg/kg
	投与経路	i.p. or s.c.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT03576963	Withdrawn	Colorectal Adenocarcinoma\|CpG Island Methylator Phenotype\|Metastatic Microsatellite Stable Colorectal Carcinoma\|Refractory Colorectal Carcinoma\|Stage IV Colorectal Cancer AJCC v8\|Stage IVA Colorectal Cancer AJCC v8\|Stage IVB Colorectal Cancer AJCC v8\|Stage IVC Colorectal Cancer AJCC v8	University of Southern California\|National Cancer Institute (NCI)\|Bristol-Myers Squibb\|Astex Pharmaceuticals Inc.	January 30 2020	Phase 1\|Phase 2
NCT03085849	Completed	Extensive-stage Small Cell Lung Cancer	Catherine Shu\|Columbia University	December 15 2017	Phase 1
NCT03179943	Active not recruiting	Urothelial Carcinoma	Fox Chase Cancer Center\|Stand Up To Cancer\|Van Andel Research Institute	November 27 2017	Phase 2
NCT02998567	Recruiting	Castration-Resistant Prostatic Cancer\|Non Small Cell Lung Cancer	Royal Marsden NHS Foundation Trust\|Astex Pharmaceuticals Inc.\|Merck Sharp & Dohme LLC\|Institute of Cancer Research United Kingdom	January 26 2017	Phase 1
NCT02892318	Completed	Acute Myeloid Leukemia	Hoffmann-La Roche	October 31 2016	Phase 1

参考
https://pubmed.ncbi.nlm.nih.gov/17616700/ https://pubmed.ncbi.nlm.nih.gov/23138873/ https://pubmed.ncbi.nlm.nih.gov/20442312/ https://pubmed.ncbi.nlm.nih.gov/31060979/ https://pubmed.ncbi.nlm.nih.gov/35843958/ + 展開

参考

https://pubmed.ncbi.nlm.nih.gov/17616700/
https://pubmed.ncbi.nlm.nih.gov/23138873/
https://pubmed.ncbi.nlm.nih.gov/20442312/

https://pubmed.ncbi.nlm.nih.gov/31060979/
https://pubmed.ncbi.nlm.nih.gov/35843958/

+ 展開

化学情報

分子量	579.39	化学式	C₁₈ H₂₃ N₉ O₁₀ P . Na
CAS No.	929904-85-8	SDF	--
Smiles	C1C(C(OC1N2C=NC3=C2N=C(NC3=O)N)COP(=O)([O-])OC4CC(OC4CO)N5C=NC(=NC5=O)N)O.[Na+]
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (172.59 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。)

Water : 50 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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