KNK437_AbMole中国_CAS号218924-25-5_M9304说明书Protocol

KNK437 目录号M9304

化学数据

分子量分子式CAS号储存条件

245.23C13H11NO4218924-25-53年 -20°C 粉末状

溶解性（25°C）

DMSO ≥ 25 mg/mLWater InsolubleEthanol N/A

生物活性

KNK437 inhibit stress-induced synthesis of heat shock proteins (HSPs). KNK437 (100 μM) inhibits thermotolerance in COLO 320DM cells after the first heat treatment. KNK437 shows inhibitory effects on thermotolerance dose-dependently in COLO 320DM cells (0-200 μM) and HeLa S3 cells (100, 200 μM).

In vivo, KNK437 (62.5-400 mg/kg) recovers bodyweight losses of tumor-free CD-1 (ICR) mice. KNK437 (200 mg/kg) alone shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors.

实验操作来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）细胞实验细胞系方法

COLO 320DM cells

Cells (1 × 105) are seeded in the flasks, incubated at 37°C for 48 h, and then heated by immersing the flasks in a water bath (45°C ± 0.05°C). KNK437 and quercetin are dissolved in DMSO before being added at the indicated concentrations. The final concentration of DMSO in each culture medium is 0.25% (v/v), irrespective of the concentrations of the drugs. The same concentration of DMSO is used as a control. Sodium arsenite is dissolved in PBS at a concentration of 80 mM and added to the medium. Cells are treated with 300 μM sodium arsenite at 37°C for 1.5 h, rinsed, and then incubated at 37°C for 5 h before 45°C heat challenge.

浓度处理时间

0, 25, 50, 100, 150, and 200 μm

动物实验动物模型配制剂量给药处理

tumor-free CD-1 (ICR) micedissolved in olive oil62.5 to 500 mg/kgi.p.

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

重量 (kg)体表面积 (m2)Km系数

0.020.0073

大鼠0.150.0256

动物B的Km系数动物A的Km系数

兔1.80.1512

豚鼠0.40.058

仓鼠0.080.025

狗100.520

动物A (mg/kg) = 动物B (mg/kg) ×

例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 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 mM5 mM10 mM

1 mg4.0778 mL0.8156 mL0.4078 mL

5 mg20.389 mL4.0778 mL2.0389 mL

10 mg40.778 mL8.1556 mL4.0778 mL

参考文献

The effects of KNK437, a novel inhibitor of heat shock protein synthesis, on the acquisition of thermotolerance in a murine transplantable tumor in vivo.

Koishi M, et al. Clin Cancer Res. 2001 Jan;7(1):215-9. PMID: 11205912.

Benzylidene lactam compound, KNK437, a novel inhibitor of acquisition of thermotolerance and heat shock protein induction in human colon carcinoma cells.

Yokota S, et al. Cancer Res. 2000 Jun 1;60(11):2942-8. PMID: 10850441.

所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务。抑制剂化合物库CCK-8 / 蛋白酶抑制剂Cocktail

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