2. Protein Tyrosine Kinase/RTK Autophagy
  3. FLT3 PDGFR Autophagy
  4. Crenolanib

Crenolanib  (Synonyms: CP-868596)

目录号: HY-13223 纯度: 99.68%
COA 产品使用指南

摩尔计算器

Crenolanib 是有效和选择性的野生型和突变型 III 类受体酪氨酸激酶抑制剂，抑制 FLT3 和 PDGFRα/β 的 Kd 分别为 0.74 nM，2.1 nM，3.2 nM。

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Crenolanib Chemical Structure

Crenolanib Chemical Structure

CAS No. : 670220-88-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥990
In-stock
1 mg ￥380
In-stock
5 mg ￥900
In-stock
10 mg ￥1500
In-stock
50 mg ￥3950
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Crenolanib:

Crenolanib 相关抗体

Top Publications Citing Use of Products

    Crenolanib purchased from MCE. Usage Cited in: Glia. 2020 Feb;68(2):345-355.  [Abstract]

    Western blots of PDGFRα and NG2 in slices treated with CP673451 and Crenolanib for 9 days.

    查看 PDGFR 亚型特异性产品:

    查看所有亚型
    PDGFR PDGFRβ PDGFRα

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

    IC50 & Target[1]

    PDGFRα

    2.1 nM (Kd)

    PDGFRβ

    3.2 nM (Kd)

    FLT3

    0.74 nM (Kd)

    体外研究
    (In Vitro)

    Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC50 values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC50 values of 93 and 26 nM, respectively[1]. HL60/VCR and K562/ABCB1 cells, overexpressing ABCB1, are 6.9- and 3.6-fold resistant to crenolanib, respectively, in relation to parental HL60 and K562 cells. PSC-833 fully reverses resistance to crenolanib in both HL60/VCR and K562/ABCB1 cells. Crenolanib (1 nM-10 μM) stimulates ABCB1 ATPase activity in a concentration-dependent manner. Crenolanib treatment does not increase the cell surface expression of ABCB1. Crenolanib inhibits [125I]-IAAP photocrosslinking of ABCB1 at high concentrations, with 50 % inhibition at 10 μM, but has little effect at lower concentrations, below 1 μM[2]. Crenolanib decreases NSCLC cell viability, induces apoptosis in NSCLC cells, and inhibits cell migration in NSCLC cells[3].

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

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

    Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice[3].

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

    443.54

    Formula

    C26H29N5O2
    CAS 号
    性状

    固体

    颜色

    Off-white to light green

    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 : 25 mg/mL (56.36 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2546 mL 11.2729 mL 22.5459 mL
    5 mM 0.4509 mL 2.2546 mL 4.5092 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% DMSO    90% Corn Oil

      Solubility: ≥ 3 mg/mL (6.76 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    • 方案 二

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

      Solubility: ≥ 1.43 mg/mL (3.22 mM); 澄清溶液

      此方案可获得 ≥ 1.43 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    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: 99.68%

    COA (198 KB) HNMR (292 KB) RP-HPLC (256 KB) LCMS (95 KB) 元素分析报告 (214 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Viable cell numbers following drug treatment are measured using the WST-1 assay. Briefly, 1×103 cells are seeded in 100 μL complete medium per well in 96-well tissue culture plates and incubated with crenolanib (0-10 μM) at 37°C in 5% CO2 for 96 h. 10 μL WST-1 reagent is then added to each well, incubation is continued for two additional hours and the color developed is quantified according to the manufacturer’s instructions. Each experiment is performed in triplicate. IC50 concentrations are calculated by the least square fit of dose–response inhibition in a non-linear regression model using GraphPad Prism V software.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    A549 cells are injected into the axillary regions of mice (2×106 cells/mouse). When the tumor volumes reached 70 mm3, the mice are randomLy allocated to the control group, low-dose crenolanib group (10 mg/kg), or high-dose crenolanib group (20 mg/kg) (n=6 per group). The vehicle for crenolanib treatment consists of 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300. The tumor size and mouse body weight are measured every other day for about 2 weeks. The tumor volume is calculated as follows: (mm3)=(width×width×length)/2. After treatment, the mice are euthanized using carbon dioxide, and the tumors are harvested and analyzed.

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

    Crenolanib 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
    DMSO 1 mM 2.2546 mL 11.2729 mL 22.5459 mL 56.3647 mL
    5 mM 0.4509 mL 2.2546 mL 4.5092 mL 11.2729 mL
    10 mM 0.2255 mL 1.1273 mL 2.2546 mL 5.6365 mL
    15 mM 0.1503 mL 0.7515 mL 1.5031 mL 3.7576 mL
    20 mM 0.1127 mL 0.5636 mL 1.1273 mL 2.8182 mL
    25 mM 0.0902 mL 0.4509 mL 0.9018 mL 2.2546 mL
    30 mM 0.0752 mL 0.3758 mL 0.7515 mL 1.8788 mL
    40 mM 0.0564 mL 0.2818 mL 0.5636 mL 1.4091 mL
    50 mM 0.0451 mL 0.2255 mL 0.4509 mL 1.1273 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:

    Crenolanib670220-88-9CP-868596CP868596CP 868596FLT3PDGFRAutophagyCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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