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  2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis
  4. Lorlatinib

Lorlatinib  (Synonyms: 勞拉替尼; PF-06463922)

目錄號: HY-12215 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

Lorlatinib (PF-06463922) 是一種具有口服活性，選擇性，腦滲透性和 ATP 競爭性的 ROS1/ALK 抑制劑，具有抗癌活性。Lorlatinib 對于 ROS1，野生型 ALK 和 ALKL1196M 的 Ki 分別為 <0.025 nM，<0.07 nM 和 0.7 nM。Lorlatinib 靶向 EML-ALK，并抑制 ALK 磷酸化，IC50 分別為 15-43 nM (ALKL1196)，14-80 nM (ALKG1269A)，38-50 nM (ALK1151Tins)，77-113 nM (ALKG1202R)。

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Lorlatinib Chemical Structure

Lorlatinib Chemical Structure

CAS No. : 1454846-35-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥858
In-stock
5 mg ￥708
In-stock
10 mg ￥1146
In-stock
25 mg ￥2488
In-stock
50 mg ￥3731
In-stock
100 mg ￥5597
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Lorlatinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 31 篇科研文獻(xiàn)

Proliferation Assay

    Lorlatinib purchased from MCE. Usage Cited in: Nat Commun. 2017 Oct 30;8(1):1197.  [Abstract]

    Representative photographs (left) and quantification (right) of soft agar colony formation assay.

    • 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

    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R), respectively[1][2][3].

    IC50 & Target

    IC50: 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R)[3]
    Ki: <0.07 nM (ALKWT), 0.6 nM (ALKL1996M), 0.9 nM (ALKG1269A), 0.1 nM (ALK1151Tins), <0.1 nM (ALKL1152R), 0.2 nM (ALKS1206Y), <0.1 nM (ALKC1156Y), <0.1nM (ALKF1174L)[3]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BaF3 IC50
    > 1000 nM
    Compound: 5
    Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    BaF3 IC50
    1.2 nM
    Compound: 5
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    BaF3 IC50
    2.9 nM
    Compound: 5
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    BaF3 IC50
    200 nM
    Compound: 5
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    BaF3 IC50
    262 nM
    Compound: 5
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    BaF3 IC50
    42.4 nM
    Compound: 5
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    HCC78 IC50
    357 nM
    Compound: 5
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    KARPAS-299 IC50
    3 nM
    Compound: 5
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    NCI-H3122 IC50
    7.8 nM
    Compound: 5
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    NIH3T3 IC50
    0.2 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    1.3 nM
    Compound: 8k, PF-06463922
    Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    1.6 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    15 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    21 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    38 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    4.2 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    77 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    NIH3T3 IC50
    9 nM
    Compound: 8k, PF-06463922
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
    		[PMID: 24819116]
    SU-DHL-1 IC50
    4.9 nM
    Compound: 5
    Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay
    		[PMID: 29288940]
    體外研究
    (In Vitro)

    Lorlatinib (PF-06463922) 對 ALK 和大量 ALK 臨床突變具有顯著的細(xì)胞活性，IC50 范圍為 0.2 nM-77 nM[1]。在攜帶 SLC34A2-ROS1 融合基因的 HCC78 人 NSCLC 細(xì)胞和表達(dá)人 CD74-ROS1 的 BaF3-CD74-ROS1 細(xì)胞中，Lorlatinib 顯著抑制細(xì)胞增殖并誘導(dǎo)細(xì)胞凋亡。Lorlatinib 還顯示出強(qiáng)大的生長抑制活性，并在攜帶非突變 ALK 或突變 ALK 融合的 NSCLC 細(xì)胞中誘導(dǎo)細(xì)胞凋亡[2]。

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

    在大鼠中，Lorlatinib (PF-06463922) 表現(xiàn)出低血漿清除率、中等分布容積、合理的半衰期、低 p-糖蛋白 1 介導(dǎo)的外排傾向和 100% 的生物利用度[1]。在體內(nèi)，Lorlatinib 通過抑制 ROS1 磷酸化和下游信號分子，以及抑制腫瘤中的細(xì)胞周期蛋白 Cyclin D1，在表達(dá)人 CD74-ROS1 和 Fig-ROS1 的 NIH3T3 異種移植模型中顯示細(xì)胞減滅性抗腫瘤功效。Lorlatinib 還在攜帶表達(dá) EML4-ALK、EML4-ALK-L1196M、EML4-ALK-G1269A、EML4-ALK-G1202R 或 NPM-ALK[2]的腫瘤異種移植物的小鼠中表現(xiàn)出顯著的抗腫瘤活性。

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

    406.41

    Formula

    C21H19FN6O2
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    勞拉替尼
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 28 mg/mL (68.90 mM; 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)

    * "≥" 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 2.4606 mL 12.3028 mL 24.6057 mL
    5 mM 0.4921 mL 2.4606 mL 4.9211 mL
    查看完整儲(chǔ)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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(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(dòng)物實(shí)驗(yàn)：

    請根據(jù)您的 實(shí)驗(yàn)動(dòng)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(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.15 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.15 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請直接配制工作液。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

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 5 mg/mL (12.30 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 0.5% CMC/saline water

      Solubility: 1 mg/mL (2.46 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請輸入動(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
    請輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(chǔ)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(chǔ)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(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(chǔ)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: 99.92%

    參考文獻(xiàn)
    Cell Assay
    [2]

    Cells are seeded in 96-well plates in growth medium containing 10% FBS and are cultured overnight at 37°C. The following day, serial dilutions of Lorlatinib or appropriate controls are added to the designated wells, and cells are incubated at 37°C for 72 h. A CellTiter-Glo assay is performed to determine the relative cell numbers. IC50 values are calculated by concentration-response curve fitting using a four-parameter analytical method.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    De novoGBM tumorigenesis is initiated in LSL-FIG-ROS1;Cdkn2a?/?;LSL-Luc mice through intracranial stereotactic injections of Adeno-Cre as described previously. Tumor development is monitored using BLI as described below. Once tumors reach a given size (107 p-1·s-1·cm-2·sr-1), animals are randomLy enrolled into vehicle control or 3-, 7-, or 14-d treatment with the indicated doses of Lorlatinib. Drug is administered through s.c. implanted Alzet osmotic pumps. After treatment, mice are killed, GBM tumors are microdissected, and tissues are flash-frozen in liquid N2. The remaining brains are processed for histology.

    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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(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 2.4606 mL 12.3028 mL 24.6057 mL 61.5142 mL
    5 mM 0.4921 mL 2.4606 mL 4.9211 mL 12.3028 mL
    10 mM 0.2461 mL 1.2303 mL 2.4606 mL 6.1514 mL
    15 mM 0.1640 mL 0.8202 mL 1.6404 mL 4.1009 mL
    20 mM 0.1230 mL 0.6151 mL 1.2303 mL 3.0757 mL
    25 mM 0.0984 mL 0.4921 mL 0.9842 mL 2.4606 mL
    30 mM 0.0820 mL 0.4101 mL 0.8202 mL 2.0505 mL
    40 mM 0.0615 mL 0.3076 mL 0.6151 mL 1.5379 mL
    50 mM 0.0492 mL 0.2461 mL 0.4921 mL 1.2303 mL
    60 mM 0.0410 mL 0.2050 mL 0.4101 mL 1.0252 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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