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Prexasertib dihydrochloride
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。
Prexasertib dihydrochloride图片
CAS NO:1234015-54-3
包装:5mg, 10mg, 25mg
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品名称
LY2606368 Prexasertib HCl
产品介绍

生物活性

Prexasertib dihydrochloride (LY2606368 HCl) 是一种有效的,ATP竞争性的选择性Chk1抑制剂,Ki值为0.9 nM,对CHK1和CHK2的IC50值分别为 <1 nM 和 8 nM。LY2606368处理将导致处于S期的细胞很快出现TUNEL和pH2AXy阳性的双链DNA断裂。在含p53缺陷的HeLa细胞中,LY2606368可有效取消doxorubicin激活的G2-M检查点,EC50为9 nM。LY2606368可广泛地在多种细胞中发挥抗增殖作用,在多数敏感细胞系中,IC50s < 50 nM;仅有少数细胞系对LY2606368具有抗性,IC50s > 1000 nM。

在体内研究中,LY2606368能有效地抑制肿瘤异种移植模型中的肿瘤生长,发挥抗肿瘤活性。在SKOV3卵巢癌模型中,LY2606368可抑制原发肿瘤的生长并显著地减少转移率和腹水积累。在SW1990原位胰脏癌模型中,LY2606368可抑制92%的原发肿瘤生长,阻止其向淋巴结结核、脾脏和肠道的转移。


化学数据

分子量438.31
分子式C18H19N7O2.2HCl
CAS号1234015-54-3
纯度>99%
溶解性(25°C)DMSO 2 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

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HeLa cells
方法HeLa cells were plated onto T25 flasks and allowed to recover for 24 hours. LY2606368 was then added to give final concentrations of 33 or 100 nmol/L. In some experiments, 20μmol/L Z-VAD-FMK was included during the drug treatment. Cells were treated for 12 hours, and during the last 2 hours, colchicine was added to 1 μg/mL. Fixation of nuclei for metaphase spreads was done following the method of Bayani and Squire. Chromosome spreads were done. A 12-μL volume of cell suspension in 3:1 methanol/acetic acid fixative was dropped from a height of 3 cm onto dry glass slides or coverslips. The slides were then heated for 45 seconds on a 43°C metal block, before being removed to allow drying to complete at room temperature. Coverslips were mounted on slides with Vectashield Hard Set mounting medium with DAPI. Slides were examined with a Leica DMR fluorescence microscope and images were captured using a SPOT RT3 Slider camera.
浓度33 or 100 nmol/L
处理时间12 h

动物实验
动物模型Female CD-1 nu-/nu- mice
配制20% Captisol, pH4
剂量15 mg/kg
给药处理s.c.

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 mM2.2815 mL11.4075 mL22.8149 mL
5 mM0.4563 mL2.2815 mL4.563 mL
10 mM0.2281 mL1.1407 mL2.2815 mL