您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PF-477736
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PF-477736
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。
PF-477736图片
CAS NO:952021-60-2
包装:2mg, 5mg, 10mg, 50mg, 100mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mM*1mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
PF-0044736
产品介绍

生物活性

PF-477736是一种有效的,选择性,ATP竞争性Chk1抑制剂,Ki为0.49 nM,也抑制VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret和Yes。作用于Chk1比作用于Chk2选择性高100倍左右。PF 477736(128 nM)作用于CA46 和 HeLa细胞,废除Camptothecin诱导的DNA损伤检查点,这种作用具有剂量依赖性。PF 477736作用于HT29细胞,有效废除Gemcitabine诱导的S期停滞,使凋亡细胞群相应增加。PF 477736(540 nM)作用于HT29细胞,增强Gemcitabine诱导的细胞毒性,这种作用具有时间和剂量依赖性。


化学数据

分子量419.48
分子式C22H25N7O2
CAS号952021-60-2
纯度99.21%
溶解性(25°C)DMSO 40 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p53-defective human cancer cell lines HT29 cells
方法IC50 MTT.
The proliferation assays were done using an MTT assay. The IC50 assay measures the antiproliferative effects of PF-00477736 on p53-defective human cancer cell lines. Cells in each line were seeded in complete medium at an exponentially growing density in 96-well assay plate and allowed to attach for 16 h. Serial dilutions of PF-00477736 were then done, and appropriate controls were added to each plate. Cells were incubated with drug for 96 h. After incubation, MTT working stock diluted in complete medium was added to each well, and cells were incubated for 4 h. After centrifugation and supernatant removal, DMSO was added to each well and plates were read on SpectraMax plate reader at 540 nm. IC50 and PF50 results were calculated by concentration-response curve fitting using a Microsoft Excel–based four-variable analysis method.
浓度0, 180, 360 and 540 n M
处理时间96 h

动物实验
动物模型Colo205 cells tumour Xenograft Models in Athymic Nude Mice
配制50 nM sodium acetate buffer and 4% dextrose (pH 4)
剂量4-60 mg/kg q3d × 4
给药处理i.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 mM2.3839 mL11.9195 mL23.839 mL
5 mM0.4768 mL2.3839 mL4.7678 mL
10 mM0.2384 mL1.192 mL2.3839 mL