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CAS No.: 2171386-10-8

RK-287107 Catalog No. CSN23902

RK-287107 is a novel tankyrase-specific inhibitor with IC50 values of 14.3 nM and 10.6 nM for tankyrase-1 and tankyrase-2, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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tech@csnpharm.cn

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述RK-287107 is a potent and highly selective TNKS1/TNKS2 inhibitor with IC50 values of 14.3nM and 10.6nM, respectively, over 190 folds of selectivity against other PARP family members at least. RK-287107 could modulate. β-catenin pathway by down-regulation of AXIN2 and TCF7 transcripts. It inhibited Wnt/β-catenin signaling pathway shown by TCF reporter assay in DLD-1 and HEK293 cells with IC50 values of 77.6 nM and 83.0 nM, respectively. Also, it inhibited human colorectal cancer Colo-320DM cell proliferation with GI50 values of 1.6μM, but not RKO cells. RK-287107 exhibited impressive pharmacokinetic profiles with rat bioavailability of approximately 60%. A tumor growth inhibition by 47.2% of mice bearing human COLO-320DM tumors could be achieved through intraperitoneal administration of 150mg/kg RK-287107 twice daily for 11 days without notable weight loss or toxicity.
动物研究
剂量
Mice: 100 mg/kg, 300 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 100 mg/kg, 300 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Mizutani A, Yashiroda Y, et al. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model. Cancer Sci. 2018;109(12):4003-4014.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4012 mL
- 12.0060 mL
- 24.0119 mL
- 5 mM
- 0.4802 mL
- 2.4012 mL
- 4.8024 mL
- 10 mM
- 0.2401 mL
- 1.2006 mL
- 2.4012 mL

技术信息

CAS号

2171386-10-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H26F2N4O2

运输

蓝冰

分子量

416.46

别名

溶解度

DMSO	83.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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