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Lorlatinib?(PF-6463922)

中文名稱：勞拉替尼

Lorlatinib (PF-6463922)是一個(gè)強(qiáng)效的，雙重 ALK/ROS1 的抑制劑，對ROS1, ALK (WT), 以及ALK (L1196M)的Ki分別為<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可誘導(dǎo)凋亡。Phase 1。

Lorlatinib?(PF-6463922) Chemical Structure

Lorlatinib?(PF-6463922) Chemical Structure

CAS: 1454846-35-5

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1285.83 現(xiàn)貨
5mg 1056.51 現(xiàn)貨
25mg 3169.53 現(xiàn)貨
100mg 4832.1 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Lorlatinib?(PF-6463922)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

ALK Signaling Pathways

ALK信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
NIH-3T3 Function assay 1 hr 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, IC50 = 0.0002 μM. 24819116
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.0012 μM. 29288940
NIH-3T3 Function assay 1 hr 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, IC50 = 0.0013 μM. 24819116
NIH-3T3 Function assay 1 hr 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, IC50 = 0.0016 μM. 24819116
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0029 μM. 29288940
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.003 μM. 29288940
NIH-3T3 Function assay 1 hr 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, IC50 = 0.0042 μM. 24819116
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay, IC50 = 0.0049 μM. 29288940
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay, IC50 = 0.0078 μM. 29288940
NIH-3T3 Function assay 1 hr 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, IC50 = 0.009 μM. 24819116
NIH-3T3 Function assay 1 hr 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, IC50 = 0.015 μM. 24819116
NIH-3T3 Function assay 1 hr 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, IC50 = 0.021 μM. 24819116
NIH-3T3 Function assay 1 hr 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, IC50 = 0.038 μM. 24819116
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.0424 μM. 29288940
NIH-3T3 Function assay 1 hr 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, IC50 = 0.077 μM. 24819116
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.2 μM. 29288940
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay, IC50 = 0.262 μM. 29288940
HCC78 Antiproliferative assay 72 hrs Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay, IC50 = 0.357 μM. 29288940
NIH/3T3 Function assay Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.0002 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.0013 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK C1156Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.0016 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.0042 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.009 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.015 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.021 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.038 μM. 28431340
NIH/3T3 Function assay Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells, IC50 = 0.077 μM. 28431340
SU-DHL1 Function assay Inhibition of ALK in human SU-DHL1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 80 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay Inhibition of ALK in human SU-DHL1 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 80 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay Inhibition of ALK phosphorylation at Y1278 residue in human SU-DHL1 cells at 20 to 80 nM after 1 hr by Western blot analysis 29288940
SU-DHL1 Function assay Inhibition of ALK in human SU-DHL1 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 80 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay Inhibition of ALK phosphorylation at Y1278 residue in human NCI-H3122 cells at 20 to 80 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay Inhibition of ALK in human NCI-H3122 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 20 to 80 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay Inhibition of ALK in human NCI-H3122 cells assessed as reduction in Akt phosphorylation at S473 residue at 20 to 80 nM after 1 hr by Western blot analysis 29288940
NCI-H3122 Function assay Inhibition of ALK in human NCI-H3122 cells assessed as reduction in ERK phosphorylation at T202//Y204 residues at 20 to 80 nM after 1 hr by Western blot analysis 29288940
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生物活性

產(chǎn)品描述 Lorlatinib (PF-6463922)是一個(gè)強(qiáng)效的，雙重 ALK/ROS1 的抑制劑，對ROS1, ALK (WT), 以及ALK (L1196M)的Ki分別為<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可誘導(dǎo)凋亡。Phase 1。
靶點(diǎn)
ROS1 [1]
(Cell-free assay)		 ALK [1]
(Cell-free assay)		 ALK (L1196M) [1]
(Cell-free assay)		 LTK (TYK1) [1]
(Cell-free assay)		 FER [1]
(Cell-free assay)		 點(diǎn)擊更多
<0.02 nM(Ki) <0.07 nM(Ki) 0.07 nM(Ki) 2.7 nM 3.3 nM
體外研究(In Vitro)
體外研究活性 PF-06463922對ALK和大量ALK臨床突變型表現(xiàn)出顯著的細(xì)胞活性，IC50范圍為0.2 nM-77 nM。[1]在含有SLC34A2-ROS1 融合物的HCC78人NSCLC細(xì)胞和表達(dá)人CD74-ROS1的BaF3-CD74-ROS1細(xì)胞中，PF-06463922顯著抑制細(xì)胞增殖，并誘導(dǎo)細(xì)胞凋亡。[2] 在含有非突變型ALK或突變型ALK融合物的NSCLC 細(xì)胞中，PF-06463922也表現(xiàn)出有效的生長抑制活性，并誘導(dǎo)細(xì)胞凋亡。[3]
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-ALK / ALK 29650534
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 在大鼠體內(nèi)，PF-06463922顯示出低血漿清除率，適度的分布容積，合理的半衰期，對低P-糖蛋白1介導(dǎo)的外排敏感性低，且生物利用度為100%。[1]在體內(nèi)，表達(dá)人CD74-ROS1 和 Fig-ROS1的NIH3T3異種移植模型中，PF-06463922表現(xiàn)出細(xì)胞減少性抗癌作用，通過抑制ROS1磷酸化和下游信號(hào)分子，以及對腫瘤中細(xì)胞周期蛋白D1的抑制發(fā)揮作用。[2]在負(fù)荷腫瘤移植物，過表達(dá)EML4-ALK，EML4-ALK-L1196M，EML4-ALK-G1269A，EML4-ALK-G1202R 或NPM-ALK的小鼠體內(nèi)，PF-06463922也表現(xiàn)出顯著的抗腫瘤活性。[3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06378892 Recruiting
Non Small Cell Lung Cancer Metastatic|ALK Gene Mutation
Centro di Riferimento Oncologico - Aviano
 March 15 2024 Phase 2
NCT06092086 Recruiting
ALK Positive Non-small Cell Lung Cancer
Guangdong Association of Clinical Trials
 August 18 2023 Phase 2
NCT05297890 Active not recruiting
Advanced or Metastatic ROS1-Positive Non-Small Cell Lung Cancer
CStone Pharmaceuticals|Pfizer
 May 27 2022 Phase 2
NCT05224609 Recruiting
Moderate Hepatic Impairment|Severe Hepatic Impairment|Healthy Volunteers
Pfizer
 April 28 2022 Phase 1

化學(xué)信息&溶解度

分子量 406.41 分子式

C21H19FN6O2
CAS號(hào) 1454846-35-5 SDF Download Lorlatinib?(PF-6463922) SDF
Smiles CC1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 81 mg/mL ( (199.3 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Ethanol : 40.5 mg/mL (99.65 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
Do you have any special suggestions for solution of S7536, Lorlatinib (PF-6463922) to be applied to mouse models?

回答：
For S7536, we recommend 2% DMSO+30% PEG 300+ddH2O (up to 5mg/ml) for in vivo application.

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