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Quizartinib

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产品编号 T2066Cas号 950769-58-1
别名 奎扎替尼, AC220

Quizartinib (AC220) 是一种第二代 Ⅱ 型 FLT3 酪氨酸激酶抑制剂,具有口服活性和高选择性,抑制 FLT3-WT 和 FLT3-ITD 自磷酸化 (IC50=4.1/1.1 nM)。Quizartinib 可以诱导肿瘤细胞凋亡。

Quizartinib

Quizartinib

Rating icon 很棒
纯度: 99.42%
产品编号 T2066 别名 奎扎替尼, AC220Cas号 950769-58-1

Quizartinib (AC220) 是一种第二代 Ⅱ 型 FLT3 酪氨酸激酶抑制剂,具有口服活性和高选择性,抑制 FLT3-WT 和 FLT3-ITD 自磷酸化 (IC50=4.1/1.1 nM)。Quizartinib 可以诱导肿瘤细胞凋亡。

规格价格库存数量
1 mg
¥ 297
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5 mg
¥ 727
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10 mg
¥ 1,080
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25 mg
¥ 1,980
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50 mg
¥ 3,250
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100 mg
¥ 4,290
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200 mg
¥ 5,970
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500 mg
¥ 8,870
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1 mL x 10 mM (in DMSO)
¥ 875
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产品介绍

生物活性
产品描述
Quizartinib (AC220) is a second-generation type II FLT3 tyrosine kinase inhibitor that is orally active and highly selective, inhibiting the autophosphorylation of FLT3-WT and FLT3-ITD (IC50=4.1/1.1 nM). Quizartinib induces apoptosis in tumor cells.
靶点活性
FLT3:1.6 nM (Kd, cell free)
体外活性
方法:人白血病细胞系 MV4-11 和人恶性黑色素瘤细胞系 A375 用 Quizartinib 处理 72 h,使用 Cell Titer-Blue Cell Viability Assay 检测细胞活力。
结果:Quizartinib 抑制 MV4-11 细胞生长,IC50 为 0.56  nM。Quizartinib 不影响 A375 细胞的增殖,IC50 大于 10000 nM。[1]
方法:AML 细胞系 MV4-11 用 Quizartinib (0.0625-8 nM) 处理 2 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:Quizartinib 对 MV4-11 细胞中的 FLT3 信号通路具有浓度依赖性抑制活性。Quizartinib 有效抑制 FLT3 磷酸化 (IC50=0.50 nM)。Quizartinib 抑制下游分子 SHP-2、STAT5、MEK1/2、ERK1/2 和 AKT的磷酸化。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Quizartinib (10 mg/kg,22% hydroxypropyl-β-cyclodextrin, CEP-701 was formulated in 20% gelucire 44/14 in water (vol/vol)) 口服给药给携带 MV4-11 异种移植物的 NU/NU 小鼠,每天一次,持续 28 天。
结果:用 10 mg/kg 的 Quizartinib 治疗导致所有动物的肿瘤快速完全消退,并且在治疗后 60 天的观察期内没有观察到肿瘤再生。[1]
激酶实验
KinomeScan kinase binding assays were performed as previously described. For the FLT3 assay, we used a kinase construct that spanned the catalytic domain only (amino acids 592 to 969 in NP_004110.2). This construct does not include the juxtamembrane domain and is designed to measure the intrinsic binding affinity of the open FLT3 active site for inhibitors [1].
细胞实验
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. 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 was added for 15 minutes after the 2-hour compound incubation. Cell lysates were prepared and incubated in 96-well plates pre-coated with a total FLT3 capture antibody. The coated plates were incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody was used for electrochemiluminescence detection on the Meso Scale Discovery platform [1].
动物实验
The model was performed according to published procedures.20 For intravenous bone marrow engraftment, nonobese diabetic/severe combined immunodeficient mice were acclimated for 2 weeks before pretreatment with 150 mg/kg cyclophosphamide delivered intraperitoneally once a day for 2 days. After a 48-hour rest period, animals were given an intravenous injection of 5 × 10^6 MV4-11 cells into the tail vein. AC220 was formulated and delivered as described for pharmacokinetic studies [1].
别名奎扎替尼, AC220
化学信息
分子量560.67
分子式C29H32N6O4S
CAS No.950769-58-1
SmilesCC(C)(C)c1cc(NC(=O)Nc2ccc(cc2)-c2cn3c(n2)sc2cc(OCCN4CCOCC4)ccc32)no1
密度1.39 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 16.67 mg/mL (29.73 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.32 mg/mL (5.92 mM), suspension.In vivo: Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
DMSO
1mg5mg10mg50mg
10 mM0.1784 mL0.8918 mL1.7836 mL8.9179 mL
20 mM0.0892 mL0.4459 mL0.8918 mL4.4590 mL

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  • 稀释 计算器
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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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