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网站主页 化工产品目录 生物化工 抑制剂 血管生成(Angiogenesis) FLT3 抑制剂 奎扎替尼 奎扎替尼
  • 奎扎替尼|T2066|TargetMol

奎扎替尼|T2066|TargetMol

Quizartinib
950769-58-1
￥297 1mg 起订
￥727 5mg 起订
￥1080 10mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
奎扎替尼
英文名称：
Quizartinib
CAS号：
950769-58-1
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.42%
产品类别：
抑制剂
货号：
T2066

Product Introduction

Bioactivity

名称Quizartinib
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.
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].
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].
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].
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]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度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. Please add co-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.
关键字AC-220 | Inhibitor | myeloid | FLT3-ITD | Apoptosis | oral | Autophagy | Fms like tyrosine kinase 3 | Target Protein-binding Moiety | mutation | inhibit | Quizartinib | CD135 | AML | leukemia | Ligands for Target Protein for PROTAC | acute | AC 220 | Cluster of differentiation antigen 135 | FLT3 | selective
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奎扎替尼|||AC220|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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