RX-3117 TV-1360; fluorocyclopentenylcytosine|cas:865838-26-2|西域试剂

RX-3117 TV-1360; fluorocyclopentenylcytosine,98.38%

产品编号：Bellancom-15228| CAS NO：865838-26-2| 分子式：C₁₀H₁₂FN₃O₄| 分子量：257.22

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货号	价格	库存与货期
Bellancom-15228	￥2300.00	杭州北京（现货）
Bellancom-15228	￥3500.00	杭州北京（现货）
Bellancom-15228	￥5000.00	杭州北京（现货）
Bellancom-15228	￥0.00	杭州北京（现货）

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RX-3117 TV-1360; fluorocyclopentenylcytosine

产品介绍

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)。

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.

体外研究

RX-3117 causes both inhibition of DNA and RNA synthesis.
RX-3117 (11.7, 21 µM; 48 h) shows antiproliferative activity in A549, SW1573 cells.
RX-3117 is activated by uridine-cytidine kinase 2 (UCK2).
RX-3117 (1-25 µM; 72 h) inhibits the growth of HCT-116, MDA-MB-231, PANC-1, Caki-1, MCF7, A549, MKN45, U251 cells with IC₅₀s of 0.39, 0.18, 0.62, 0.84, 0.34, 0.34, 0.50, 0.83 µM, respectively.
RX-3117 (5, 10 µM; 4 days) induces cell cycle arrest at S phase and apoptosis.
RX-3117 (1-5 µM; 24 h) decreases the cellular amount of DNMT1 in a dose-dependent manner in MDA-MB-231.

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

Cell Viability Assay

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

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; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice.

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

Animal Model:	Nude mice (human colon carcinoma HCT116 xenograft model)
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.

体内研究

RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice.

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

Animal Model:	Nude mice (human colon carcinoma HCT116 xenograft model)
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.

体内研究

RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice.

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

Animal Model:	Nude mice (human colon carcinoma HCT116 xenograft model)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (194.39 mM)

* "≥" 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

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, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式