2. Protein Tyrosine Kinase/RTK PROTAC Apoptosis
  3. FLT3 Ligands for Target Protein for PROTAC Apoptosis
  4. Quizartinib

Quizartinib  (Synonyms: 奎扎替尼; AC220; AC708)

目录号: HY-13001 纯度: 98.83%
COA 产品使用指南

摩尔计算器

Quizartinib (AC220) 是一种具有口服活性的、高选择性的，有效的第二代 Ⅱ 型 FLT3 (type II FLT3) 酪氨酸激酶抑制剂，Kd 值为 1.6 nM。Quizartinib 抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化，IC50 分别为 4.1 nM 和 1.1 nM。Quizartinib 可以通过优化的 linker 与 VHL 配体连接，从而形成 PROTAC Flt3 降解剂。Quizartinib 诱导细胞凋亡 (apoptosis)。

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Quizartinib Chemical Structure

Quizartinib Chemical Structure

CAS No. : 950769-58-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1172
In-stock
1 mg ￥380
In-stock
5 mg ￥909
In-stock
10 mg ￥1350
In-stock
25 mg ￥2450
In-stock
50 mg ￥3920
In-stock
100 mg ￥5200
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Quizartinib:

Quizartinib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 31 篇科研文献

WB

    Quizartinib purchased from MCE. Usage Cited in: J Med Chem. 2017 Oct 26;60(20):8407-8424.  [Abstract]

    Doseresponsive immunoblotting of the signaling pathway with the cells extracted from tumor tissues of the experimental animal after the 14 and 7 (AC220) treatments.

    Quizartinib purchased from MCE. Usage Cited in: Oncotarget. 2016 Jul 26;7(30):47018-47032.  [Abstract]

    A. The established 32D cells are treated with Quizartinib for 2h, followed by 10 ng/mL FL stimulation for 10 minutes. Wt-FLT3 and mutant FLT3 are immunoprecipitated by each tag as indicated and subjected to Western blot. Phosphorylation levels of FLT3, STAT5, AKT and MAPK are examined. B. 32D cells are treated with Quizartinib at the indicated concentrations in the presence or absence of 10 ng/mL FL for 2 hours. Phosphorylation levels of FLT3, STAT5, AKT and MAPK are detected by Western blot.

    Quizartinib purchased from MCE. Usage Cited in: Cancer Cell. 2014 Feb 10;25(2):226-42.  [Abstract]

    Western blot for indicated proteins on lysates from FLT3-ITD-positive primary murine cells expressing either wild-type (WT) or constitutive active (SYK-TEL) SYK and treated for eight hours with indicated doses of AC220.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis[1].

    IC50 & Target

    Kd: 1.6±0.7 nM (Flt3)[1]
    体外研究
    (In Vitro)

    Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56±0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Quizartinib 相关抗体:
    体内研究
    (In Vivo)

    Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    560.67

    Formula

    C29H32N6O4S
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    奎扎替尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (58.86 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    DMF 中的溶解度 : 10 mg/mL (17.84 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7836 mL 8.9179 mL 17.8358 mL
    5 mM 0.3567 mL 1.7836 mL 3.5672 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMF    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (1.78 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂： 10% DMF    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1 mg/mL (1.78 mM); 澄清溶液

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.01%

    COA (284 KB) HNMR (182 KB) RP-HPLC (240 KB) 元素分析报告 (206 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    KinomeScan kinase binding assays are performed. For the FLT3 assay, a kinase construct that spanned the catalytic domain only (amino acids 592 to 969) is used. 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    MV4-11 and RS4;11 cells are cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells are cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors (e.g., Quizartinib) are added to the cells and incubated at 37°C for 72 hours. Cell viability is measured using the Cell Titer-Blue Cell Viability Assay. To measure inhibition of FLT3 autophosphorylation, cells are 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 are incubated with inhibitors (e.g., Quizartinib) for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand is added for 15 minutes after the 2-hour compound incubation. Cell lysates are prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody. The coated plates are 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 is used for electrochemiluminescence detection on the Meso Scale Discovery platform[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Female NU/NU or severe combined immunodeficient mice are used. Quizartinib (hydrochloride salt) is formulated in 22% hydroxypropyl-β-cyclodextrin, CEP-701 is formulated in 20% gelucire 44/14 in water (vol/vol), MLN-518 and SU 11248 are formulated in 10 mM sodium citrate (pH 3.5), PKC-412 is formulated in 3:1 gelucire 44/14-propylene glycol (vol/vol), and Bay 43-9006 is formulated in 80% PEG-400. Compound concentrations are chosen to deliver the desired dose in a volume of 10 mL/kg. Compounds are administered by oral gavage and plasma samples collected 0.25, 0.5, 1, 2, 4, 6, and 24 hours after dosing. To collect plasma samples, eye bleeds (150 μL) are taken semilongitudinally using 3 groups of 3 animals each, taking 2 to 3 time points per animal to obtain a total of 3 independent plasma concentration time courses. Plasma samples and controls (25 μL) are extracted with 4 volumes of acetonitrile containing an internal standard and analyzed by liquid chromatography tandem mass spectrometry.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Quizartinib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMF / DMSO 1 mM 1.7836 mL 8.9179 mL 17.8358 mL 44.5895 mL
    5 mM 0.3567 mL 1.7836 mL 3.5672 mL 8.9179 mL
    10 mM 0.1784 mL 0.8918 mL 1.7836 mL 4.4590 mL
    15 mM 0.1189 mL 0.5945 mL 1.1891 mL 2.9726 mL
    DMSO 20 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2295 mL
    25 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7836 mL
    30 mM 0.0595 mL 0.2973 mL 0.5945 mL 1.4863 mL
    40 mM 0.0446 mL 0.2229 mL 0.4459 mL 1.1147 mL
    50 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Quizartinib950769-58-1AC220 AC708奎扎替尼AC 220AC-220AC708AC 708AC-708FLT3Ligands for Target Protein for PROTACApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Target Protein-binding MoietyoralselectiveAMLacutemyeloidleukemiaFLT3-ITDmutationInhibitorinhibitorinhibit

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