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AC220
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。
AC220图片
CAS NO:950769-58-1
包装:5mg, 10mg
包装与价格:
包装价格(元)
10mM*1mL in DMSO电议
5mg电议
10mg电议

产品名称
Quizartinib
产品介绍

生物活性

Quizartinib (AC220)是一种二代FLT3抑制剂,作用于Flt3(ITD/WT),IC50为1.1 nM/4.2 nM,作用于Flt3比作用于KIT, PDGFRA, PDGFRB, RET,和CSF-1R选择性高10倍。AC220是最有效的FLT3选择性抑制剂,可用于治疗急性骨髓性白血病(AML)。AC220在生化和细胞实验中具有低纳摩尔效果和特别的激酶选择性,抑制大部分人类蛋白激酶时具有高选择性。AC220是治疗急性骨髓性白血病(AML)的新型FLT3抑制剂。


化学数据

分子量560.67
分子式C29H32N6O4S
CAS号950769-58-1
纯度>98%
溶解性(25°C)DMSO ≥100 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MV4-11 and RS4;11 cells
方法Cellular assays. MV4-11 and RS4;11 cells were cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells were cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors were added to the cells and incubated at 37°C for 72 hours. Cell viability was measured using the Cell Titer-Blue Cell Viability Assay from Promega. To measure inhibition of FLT3 autophosphorylation, cells were cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells were incubated with inhibitors for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand (R&D Systems) was added for 15 minutes after the 2-hour compound incubation. Cell lysates were prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody (R&D Systems). The coated plates were incubated with either a biotinylated antibody against FLT3 (R&D Systems) to detect total FLT3 or an antibody against phosphotyrosines (Millipore) to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody was used for electrochemiluminescence detection on the Meso Scale Discovery platform.
浓度0~10 μM
处理时间72 h

动物实验
动物模型subcutaneous tumor model
配制22% hydroxypropyl-β-cyclodextrin
剂量10 mg/kg
给药处理orally

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 mM1.7836 mL8.9179 mL17.8358 mL
5 mM0.3567 mL1.7836 mL3.5672 mL
10 mM0.1784 mL0.8918 mL1.7836 mL