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Tucidinostat(Chidamide)HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tucidinostat(Chidamide)HCl图片
CAS NO:743420-02-2

产品名称
Chidamide
HBI-8000
CS-055 HCl
产品介绍

生物活性

Tucidinostat (HBI-8000; Chidamide; CS-055) HCl is a benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10 with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. Tucidinostat selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. This agent also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis.

In vivo, Chidamide shows in vivo antitumor activity in HCT-8 colorectal carcinoma mice xenografts. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss.


化学数据

分子量463.33
分子式C22H21Cl2FN4O2
CAS号743420-02-2
纯度>98.5%
溶解性(25°C)DMSO ≥ 60 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.1583 mL10.7914 mL21.5829 mL
5 mM0.4317 mL2.1583 mL4.3166 mL
10 mM0.2158 mL1.0791 mL2.1583 mL