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  2. Protein Tyrosine Kinase/RTK Autophagy
  3. Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy
  4. Crizotinib hydrochloride

Crizotinib hydrochloride  (Synonyms: PF-02341066 hydrochloride)

目錄號(hào): HY-50878A 純度: 99.80%
COA 產(chǎn)品使用指南 技術(shù)支持

Crizotinib hydrochloride (PF-02341066 hydrochloride) 是一種口服生物可用的，具有選擇性的 ATP 競(jìng)爭(zhēng)性雙 ALK 和 c-Met 抑制劑，IC50 分別為 20 和 8 nM。在細(xì)胞的實(shí)驗(yàn)中，Crizotinib hydrochloride (PF-02341066 hydrochloride) 抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化，IC50 分別為 24 和 11 nM。它也是 ROS 原癌基因 1 (ROS1) 抑制劑。Crizotinib hydrochloride (PF-02341066 hydrochloride) 具有有效的腫瘤生長(zhǎng)抑制作用。

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Crizotinib hydrochloride Chemical Structure

Crizotinib hydrochloride Chemical Structure

CAS No. : 1415560-69-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥397
In-stock
5 mg ￥371
In-stock
10 mg ￥590
In-stock
25 mg ￥854
In-stock
50 mg ￥1196
In-stock
100 mg ￥1680
In-stock
200 mg ￥2100
In-stock
500 mg ￥2900
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Crizotinib hydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 68 篇科研文獻(xiàn)

WB

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2019 Nov 7;2019:4253846.  [Abstract]

    Western blot analysis of cleaved caspase 3, Bax, and Bcl-2 expression after serum-free culture for 72 h with or without Crizotinib.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: J Hematol Oncol. 2018 Aug 29;11(1):109.  [Abstract]

    Resistant cells are treated with 200 nM Afatinib alone or in combination with 1 μM Crizotinib for 48 h.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.  [Abstract]

    At 50mg/kg, Crizotinib inhibits MET phosphorylation and downstream signaling pathway activation.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2018 May 28;422:19-28.  [Abstract]

    CD74-ROS1 or CD74-ROS1 G2032R mutation cells are treated with Crizotinib for 24?h, the expression of ROS1 or p-ROS1 is determined by western blot.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):996-1006.  [Abstract]

    Dose-response and time course comparison of ALK inhibition by Crizotinib or Ceritinib.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Dis Model Mech. 2016 Sep 1;9(9):941-52.  [Abstract]

    CLB-BAR, CLB-GE neuroblastoma cells are treated for 6 h with either Crizotinib or PF-04643922. Cells are harvested and pre-cleared cell lysates are analyzed on SDS PAGE followed by western blotting for ALK, phospho-ALK-Y1278, phospho-ERK5, pan-ERK5 phospho-ERK1/2 and pan-ERK. Actin is employed as a loading control. Protein band intensities are quantified by Image Studio Lite 3.1 and normalized to untreated samples.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2016 May 17;7(20):29011-22.  [Abstract]

    A, B. CLB-BAR (ALK-Δ4-11) and CLB-GE (ALK-F1174V), both ALK addicted cell lines, are treated with increasing doses of Brigatinib for 6 hours. Crizotinib (250 nM) is employed as a positive control. Cells lysates are resolved on SDS/PAGE followed by immunoblotting for pALK (Y1604) and additional downstream targets as indicated.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102.  [Abstract]

    Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.

    Crizotinib hydrochloride purchased from MCE. Usage Cited in: Oncotarget. 2014 May 15;5(9):2688-702.  [Abstract]

    The Ret expression level is investigated by Western blot in MYCN/KI AlkR1279Q and MYCN/KI AlkF1178L treated tumors and controls using the anti-Ret antibody EPR2871. Actin is used as a standard for quantification.

    • 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

    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition[1][2][3].

    IC50 & Target

    IC50: 20 nM (ALK), 8 nM (c-Met)[3]
    體外研究
    (In Vitro)

    PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively[1].
    PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    PF-2341066 reveals the ability to cause marked regression of large established tumors (> 600 mm3) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule in the GTL-16 model. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. A significant dose-dependent reduction of CD31-positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066[1].
    Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1[4].

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

    486.80

    Formula

    C21H23Cl3FN5O
    CAS 號(hào)
    性狀

    固體

    顏色

    Yellow to brown

    中文名稱

    克里唑替尼鹽酸
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    H2O 中的溶解度 : 50 mg/mL (102.71 mM; 超聲助溶)

    DMSO 中的溶解度 : ≥ 4.9 mg/mL (10.07 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.0542 mL 10.2712 mL 20.5423 mL
    5 mM 0.4108 mL 2.0542 mL 4.1085 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 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(dòng)物實(shí)驗(yàn)：

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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(qǐng)依序添加每種溶劑： PBS

      Solubility: 55 mg/mL (112.98 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.86%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Tumor cells are seeded in 96-well plates at low density in media supplemented with 10% FBS (growth media) and transferred to serum-free media (0% FBS and 0.04% BSA) after 24 h. Appropriate controls or designated concentrations of PF-2341066 are added to each well, and cells are incubated for 24 to 72 h. Human umbilical vascular endothelial cells (HUVEC) are seeded in 96-well plates in EGM2 media for 5 to 6 h at > 20,000 cells per well and transferred to serum-free media overnight. The following day, appropriate controls or designated concentrations of PF-2341066 are added to each well, and after 1 h incubation, HGF is added to designated wells at 100 ng/mL. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay is done to determine the relative tumor cell or HUVEC numbers.

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

    Athymic mice bearing xenografts (300-800 mm3) are given PF-2341066 in water by oral gavage at designated dose levels. At designated times following PF-2341066 administration, mice are humanely euthanized, and tumors are resected. Tumors are snap frozen and pulverized using a liquid nitrogen-cooled cryomortar and pestle, protein lysates are generated, and protein concentrations are determined using a BSA assay. The level of total and phosphorylated protein is determined using a capture ELISA or immunoprecipitation-immunoblotting method.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)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 / H2O 1 mM 2.0542 mL 10.2712 mL 20.5423 mL 51.3558 mL
    5 mM 0.4108 mL 2.0542 mL 4.1085 mL 10.2712 mL
    10 mM 0.2054 mL 1.0271 mL 2.0542 mL 5.1356 mL
    H2O 15 mM 0.1369 mL 0.6847 mL 1.3695 mL 3.4237 mL
    20 mM 0.1027 mL 0.5136 mL 1.0271 mL 2.5678 mL
    25 mM 0.0822 mL 0.4108 mL 0.8217 mL 2.0542 mL
    30 mM 0.0685 mL 0.3424 mL 0.6847 mL 1.7119 mL
    40 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2839 mL
    50 mM 0.0411 mL 0.2054 mL 0.4108 mL 1.0271 mL
    60 mM 0.0342 mL 0.1712 mL 0.3424 mL 0.8559 mL
    80 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6419 mL
    100 mM 0.0205 mL 0.1027 mL 0.2054 mL 0.5136 mL

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    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：
    Crizotinib hydrochloride
    目錄號(hào)：
    HY-50878A
    需求量：