RX-3117 (Synonyms: TV-1360; Fluorocyclopentenylcytosine)

目录号: HY-15228 纯度: ≥98.0%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

RX-3117 (TV-1360) 是一种有效的口服活性抗癌和抗代谢物药剂。RX-3117 抑制 DNA 甲基转移酶 1 (DNMT1。RX-3117 显示出抗增殖和抗肿瘤活性。RX-3117 诱导细胞周期停滞在 S 期和细胞凋亡 (apoptosis)。

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RX-3117 Chemical Structure

CAS No. : 865838-26-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3850	In-stock
1 mg	￥1600	In-stock
2 mg	￥2300	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

•bioRxiv. 2023.

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生物活性
纯度 & 产品资料
参考文献

生物活性

RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis^[1]^[2]^[3].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.5 μM Compound: 5a	Antitumor activity against human A549 cells by SRB method Antitumor activity against human A549 cells by SRB method	[PMID: 22524616]
HCT-116	IC₅₀	0.19 μM Compound: 5a	Antitumor activity against human HCT116 cells by SRB method Antitumor activity against human HCT116 cells by SRB method	[PMID: 22524616]
HeLa	IC₅₀	1.35 μM Compound: 5a	Antitumor activity against human HeLa cells by SRB method Antitumor activity against human HeLa cells by SRB method	[PMID: 22524616]
HepG2	IC₅₀	0.79 μM Compound: 5a	Antitumor activity against human HepG2 cells by SRB method Antitumor activity against human HepG2 cells by SRB method	[PMID: 22524616]
HT-29	IC₅₀	0.28 μM Compound: 5a	Antitumor activity against human HT-29 cells by SRB method Antitumor activity against human HT-29 cells by SRB method	[PMID: 22524616]
K562	IC₅₀	0.82 μM Compound: 5a	Antitumor activity against human K562 cells by SRB method Antitumor activity against human K562 cells by SRB method	[PMID: 22524616]
LNCaP	IC₅₀	2.67 μM Compound: 5a	Antitumor activity against human LNCAP cells by SRB method Antitumor activity against human LNCAP cells by SRB method	[PMID: 22524616]
MCF7	IC₅₀	0.34 μM Compound: 5a	Antitumor activity against human MCF7 cells by SRB method Antitumor activity against human MCF7 cells by SRB method	[PMID: 22524616]
MDA-MB-231	IC₅₀	0.18 μM Compound: 5a	Antitumor activity against human MDA-MB-231 cells by SRB method Antitumor activity against human MDA-MB-231 cells by SRB method	[PMID: 22524616]
MKN-45	IC₅₀	0.34 μM Compound: 5a	Antitumor activity against human MKN45 cells by SRB method Antitumor activity against human MKN45 cells by SRB method	[PMID: 22524616]
NCI-H226	IC₅₀	0.25 μM Compound: 5a	Antitumor activity against human NCI-H226 cells by SRB method Antitumor activity against human NCI-H226 cells by SRB method	[PMID: 22524616]
OVCAR-3	IC₅₀	0.8 μM Compound: 5a	Antitumor activity against human OVCAR3 cells by SRB method Antitumor activity against human OVCAR3 cells by SRB method	[PMID: 22524616]
PANC-1	IC₅₀	0.62 μM Compound: 5a	Antitumor activity against human PANC1 cells by SRB method Antitumor activity against human PANC1 cells by SRB method	[PMID: 22524616]
PC-3	IC₅₀	0.63 μM Compound: 5a	Antitumor activity against human PC3 cells by SRB method Antitumor activity against human PC3 cells by SRB method	[PMID: 22524616]
SK-MEL-28	IC₅₀	1.38 μM Compound: 5a	Antitumor activity against human SK-MEL-28 cells by SRB method Antitumor activity against human SK-MEL-28 cells by SRB method	[PMID: 22524616]
U-251	IC₅₀	0.83 μM Compound: 5a	Antitumor activity against human U251 cells by SRB method Antitumor activity against human U251 cells by SRB method	[PMID: 22524616]

体外研究
(In Vitro)

RX-3117 抑制 DNA 和 RNA 合成^[1]。
RX-3117 (11.7，21 μM；48 小时) 在 A549、SW1573 细胞中表现出抗增殖活性^[1]。
RX-3117 被尿苷胞苷激酶 2 (UCK2) 激活^[1]。
RX-3117 (1-25 μM；72 h) 抑制 HCT-116、MDA-MB-231、PANC-1、Caki-1、MCF7、A549、MKN45、U251 细胞的生长，IC₅₀ 分别为 0.39、0.18、0.62，分别为 0.84、0.34、0.34、0.50、0.83 μM^[2]。
RX-3117 (5、10 μM；4 天) 诱导细胞周期停滞在 S 期和细胞凋亡^[2]。
RX-3117 (1-5 μM；24 小时) 在 MDA-MB-231 中以剂量依赖性方式降低 DNMT1 的细胞量^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	A549, SW1573 cells
Concentration:	11.7, 21 µM
Incubation Time:	48 h
Result:	Showed antiproliferative activity in A549 (63.7% cell growth), SW1573 cells (59% cell growth).

Apoptosis Analysis^[2]

Cell Line:	A549, SW1573 NSCLC cells
Concentration:	5 µM for A549 cells, 10 µM for SW1573 cells
Incubation Time:	4 days
Result:	Induced cell cycle arrest at S phase and apoptosis.

体内研究
(In Vivo)

RX-3117 (2，10 mg/kg；腹腔注射；每周 3 次，持续 5 周) 在裸鼠体内显示出抗肿瘤活性^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice (human colon carcinoma HCT116 xenograft model)^[3]
Dosage:	2, 10 mg/kg
Administration:	I.p.; three times per week for five weeks
Result:	Caused significant inhibition of tumor growth at the doses of 2 and 10 mg/kg.

Clinical Trial

分子量

257.22

Formula

C₁₀H₁₂FN₃O₄

CAS 号

865838-26-2

性状

固体

颜色

White to off-white

中文名称

氟环戊烯基胞嘧啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (194.39 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8877 mL	19.4386 mL	38.8772 mL
5 mM	0.7775 mL	3.8877 mL	7.7754 mL
10 mM	0.3888 mL	1.9439 mL	3.8877 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: ≥98.0%

选择批次：

Data Sheet (617 KB) SDS (252 KB)

COA (195 KB) HNMR (248 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Sarkisjan D, et al. The Cytidine Analog Fluorocyclopentenylcytosine (RX-3117) Is Activated by Uridine-Cytidine Kinase 2. PLoS One. 2016 Sep 9;11(9):e0162901. [Content Brief]

[2]. Balboni B, et al. RX-3117 (fluorocyclopentenyl cytosine): a novel specific antimetabolite for selective cancer treatment. Expert Opin Investig Drugs. 2019 Apr;28(4):311-322. [Content Brief]

[3]. Fahy J, et al. DNA methyltransferase inhibitors in cancer: a chemical and therapeutic patent overview and selected clinical studies. Expert Opin Ther Pat. 2012 Dec;22(12):1427-42. [Content Brief]

RX-3117 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.8877 mL	19.4386 mL	38.8772 mL	97.1931 mL
	5 mM	0.7775 mL	3.8877 mL	7.7754 mL	19.4386 mL
	10 mM	0.3888 mL	1.9439 mL	3.8877 mL	9.7193 mL
	15 mM	0.2592 mL	1.2959 mL	2.5918 mL	6.4795 mL
	20 mM	0.1944 mL	0.9719 mL	1.9439 mL	4.8597 mL
	25 mM	0.1555 mL	0.7775 mL	1.5551 mL	3.8877 mL
	30 mM	0.1296 mL	0.6480 mL	1.2959 mL	3.2398 mL
	40 mM	0.0972 mL	0.4860 mL	0.9719 mL	2.4298 mL
	50 mM	0.0778 mL	0.3888 mL	0.7775 mL	1.9439 mL
	60 mM	0.0648 mL	0.3240 mL	0.6480 mL	1.6199 mL
	80 mM	0.0486 mL	0.2430 mL	0.4860 mL	1.2149 mL
	100 mM	0.0389 mL	0.1944 mL	0.3888 mL	0.9719 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

RX-3117 (Synonyms: TV-1360; Fluorocyclopentenylcytosine)

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献