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

Crenolanib  (Synonyms: CP-868596)

目錄號: HY-13223 純度: 99.68%
COA 產(chǎn)品使用指南

Crenolanib 是有效和選擇性的野生型和突變型 III 類受體酪氨酸激酶抑制劑,抑制 FLT3PDGFRα/βKd 分別為 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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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥990
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1 mg ¥380
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5 mg ¥900
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10 mg ¥1500
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50 mg ¥3950
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100 mg 現(xiàn)貨 詢價
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Customer Review

Other Forms of Crenolanib:

    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 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    體外研究
    (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.

    體內(nèi)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 號
    性狀

    固體

    顏色

    Off-white to light green

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 25 mg/mL (56.36 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請?jiān)?年內(nèi)使用, -20°C儲存時,請?jiān)?個月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    90% Corn Oil

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

      此方案可獲得 ≥ 3 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 30.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

    • 方案 二

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 1.43 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 14.3 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
    連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.68%

    參考文獻(xiàn)
    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.

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時,請?jiān)?年內(nèi)使用, -20°C儲存時,請?jiān)?個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    產(chǎn)品名稱:
    Crenolanib
    目錄號:
    HY-13223
    需求量: