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3-arylisoquinolinamine derivative

产品编号 T10106 CAS 1029008-71-6

3-arylisoquinolinamine derivative is a compound with antitumor activity.

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3-arylisoquinolinamine derivative Chemical Structure

3-arylisoquinolinamine derivative, CAS 1029008-71-6

规格	价格/CNY	货期
2 mg	￥ 495	5日内发货
5 mg	￥ 828	5日内发货
10 mg	￥ 1,620	5日内发货
100 mg	￥ 7,320	6-8周
1 mL * 10 mM (in DMSO)	￥ 913	5日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	3-arylisoquinolinamine derivative is a compound with antitumor activity.
靶点活性	SK-MEL-28 cells:32 nM , Colon HCT 116 cells:17 nM , MDA-MB-231 cells:21 nM , Pancreas PANC-1:19 nM , Kidney Caki-1:22 nM , OVCAR-3 (ovary):14 nM , SNB19 (Glioblastoma):32 nM , Prostate PC3:19 nM
体外活性	3-arylisoquinolinamine derivative (7b) shows more effective activity against Paclitaxel-resistant HCT-15 human colorectal cancer cell lines when compared to the original cytotoxic cancer drug, Paclitaxel. The cell cycle dynamics is analyzed by flow cytometry. Treatment of human HCT-15 cells with 3-arylisoquinolinamine derivative (7b) blocks or delays the progression of cells from the G0/G1 phase into the S phase, and induces cell death. 3-arylisoquinolinamine derivative (7b) inhibits the cell growth (IC50: 14 nM to 32 nM). In cell cycle analysis using HCT-15 cells, the treatment of 1 nM of 3-arylisoquinolinamine derivative (7b) displays a significant increase in G0/G1 phase at 24 h with a decrease in G2/M phase, but the increase of G0/G1 phase at 48 h is not significant. At a higher concentration of 3-arylisoquinolinamine derivative (7b) (10 nM), there are a significant increase in G0/G1 phase and a decrease in G2/M phase, and the emergence of sub-G1phase, at both 24 h and 48 h. 3-arylisoquinolinamine derivative (7b) blocks or delays the progression of cells from the G0/G1 phase into S phase, and induces cell death [1]. 3-arylisoquinolinamine derivative (compound 13; IC50: 15 nM in HCT-15 cells, 17 nM in HCT116 cells) shows potent antiproliferative activities with IC50 value in the low nanomolar range in both cells and higher antitumor activities than that of Paclitaxel against Paclitaxel-resistant HCT-15 colorectal cancer cells [2].
体内活性	3-arylisoquinolinamine derivative has higher antitumor efficacy (69.2 % inhibition) than that of the control drug, Paclitaxel (48.8 % inhibition) in the inhibition of growth of tumor in an animal model [2].
动物实验	The six-week-old female athymic mice (BALB/c nu/nu) are used. All study medications (vehicle control, Paclitaxel: 10 mg/kg/day, 3-arylisoquinolinamine derivative: 10 mg/kg/day) are given by intraperitoneal injections three times per week starting from day 10 and ending on day 29 after inoculation of HCT 15 cells. To quantify tumor growth, three perpendicular diameters of the tumors are measured with calipers every 3-5 days, and the bodyweight of the mice was monitored for toxicity. The tumor volume is calculated [2].

分子量	293.36
分子式	C18H19N3O
CAS No.	1029008-71-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (170.44 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4088 mL	17.0439 mL	34.0878 mL	85.2195 mL
	5 mM	0.6818 mL	3.4088 mL	6.8176 mL	17.0439 mL
	10 mM	0.3409 mL	1.7044 mL	3.4088 mL	8.522 mL
	20 mM	0.1704 mL	0.8522 mL	1.7044 mL	4.261 mL
	50 mM	0.0682 mL	0.3409 mL	0.6818 mL	1.7044 mL
	100 mM	0.0341 mL	0.1704 mL	0.3409 mL	0.8522 mL

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参考文献

1. Yang SH, et al. Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5277-81. 2. Young Bok Lee, et al. 5, 6, or 7-substituted-s- (hetero)arylisoquinolinamine derivatives as antitumor agents. WO 2008063548 A2.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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