Entrectinib
别名: RXDX-101, NMS-E628 中文名称：恩曲替尼
Entrectinib是一种口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制剂，IC50范围为 0.1~1.7 nM。Entrectinib (RXDX-101) 可诱导自噬。Phase 2。
Entrectinib Chemical Structure
CAS: 1108743-60-7
客户使用Selleck的Entrectinib发表文献41篇
产品质控
Entrectinib相关产品
| 相关靶点 | TrkA TrkB TrkC | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
相关信号通路图
Trk receptor抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| KARPAS299 | Function assay | 60 mg/kg | 12 hrs | Ex vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis | 27003761 |
| KARPAS299 | Function assay | 60 mg/kg | 18 hrs | Ex vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis | 27003761 |
| KARPAS299 | Function assay | 60 mg/kg | 12 hrs | Ex vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells assessed as suppression of STAT3 phosphorylation at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis | 27003761 |
| KARPAS299 | Function assay | 60 mg/kg | 18 hrs | In vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells assessed as suppression of STAT3 phosphorylation at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis | 27003761 |
| NCI-H2228 | Antitumor assay | 30 to 60 mg/kg | 10 days | Antitumor activity against human NCI-H2228 cells xenografted in athymic nu/nu mouse assessed as tumor growth inhibition at 30 to 60 mg/kg, po bid administered for 10 days | 27003761 |
| NCI-H2228 | Function assay | 60 mg/kg | 12 hrs | Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis | 27003761 |
| NCI-H2228 | Function assay | 60 mg/kg | 18 hrs | Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis | 27003761 |
| NCI-H2228 | Function assay | 60 mg/kg | 12 hrs | Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells assessed as suppression of AKT phosphorylation at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis | 27003761 |
| NCI-H2228 | Function assay | 60 mg/kg | 18 hrs | Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells assessed as suppression of AKT phosphorylation at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis | 27003761 |
| KARPAS299 | Antitumor assay | 30 to 60 mg/kg | 10 days | Antitumor activity against human KARPAS299 cells xenografted in SCID mouse assessed as tumor growth inhibition at 30 to 60 mg/kg, po bid administered for 10 days | 27003761 |
| KARPAS299 | Antitumor assay | 30 to 60 mg/kg | 10 days | Antitumor activity against human KARPAS299 cells xenografted in SCID mouse assessed as tumor free cured mouse at 30 to 60 mg/kg, po bid administered for 10 days measured on day 90 | 27003761 |
| BAF3 | Function assay | 72 hrs | Inhibition of human TEL (336 residues) fused-ROS1 (1891 to 2347 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.005 μM. | 27003761 | |
| BAF3 | Function assay | 72 hrs | Inhibition of human TEL (336 residues) fused-TRKC (454 to 825 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.003 μM. | 27003761 | |
| BAF3 | Function assay | 72 hrs | Inhibition of human TEL (336 residues) fused-TRKA (440 to 796 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.003 μM. | 27003761 | |
| BAF3 | Function assay | 72 hrs | Inhibition of human TEL (336 residues) fused-TRKB (455 to 822 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.003 μM. | 27003761 | |
| KM12 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KM12 cells expressing TRKA protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.017 μM. | 27003761 | |
| SU-DHL1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SU-DHL1 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.024 μM. | 27003761 | |
| BAF3 | Function assay | 72 hrs | Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.028 μM. | 27003761 | |
| KARPAS299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KARPAS299 cells incubated for 72 hrs by cell titer-glo assay, IC50 = 0.031 μM. | 27003761 | |
| SUP-M2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SUP-M2 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.041 μM. | 27003761 | |
| BAF3 | Function assay | 72 hrs | Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.067 μM. | 27003761 | |
| NCI-H2228 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H2228 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.068 μM. | 27003761 | |
| MV411 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV411 cells incubated for 72 hrs by cell titer-glo assay, IC50 = 0.081 μM. | 27003761 | |
| SR786 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SR786 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.081 μM. | 27003761 | |
| BAF3 | Function assay | 72 hrs | Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.897 μM. | 27003761 | |
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse IL-3 dependent BA/F3 cells incubated for 72 hrs by cell titer-glo assay, IC50 = 2.104 μM. | 27003761 | |
| KM12 | Function assay | 2 hrs | Inhibition of TPM3-TRKA phosphorylation in human KM12 cells at low concentration after 2 hrs by Western blot analysis | 27003761 | |
| KM12 | Function assay | 2 hrs | Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of MAPK phosphorylation at low concentration after 2 hrs by Western blot analysis | 27003761 | |
| KM12 | Function assay | 2 hrs | Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of PLCgamma1 phosphorylation at low concentration after 2 hrs by Western blot analysis | 27003761 | |
| KM12 | Function assay | 2 hrs | Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of AKT phosphorylation at low concentration after 2 hrs by Western blot analysis | 27003761 | |
| KM12 | Function assay | 2 hrs | Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of S6 phosphorylation at low concentration after 2 hrs by Western blot analysis | 27003761 | |
| KARPAS299 | Function assay | 2 hrs | Inhibition of NPM/ALK autophosphorylation in human KARPAS299 cells at very low concentration after 2 hrs by Western blot analysis | 27003761 | |
| NCI-H2228 | Function assay | 2 hrs | Inhibition of NPM/ALK autophosphorylation in human NCI-H2228 cells at very low concentration after 2 hrs by Western blot analysis | 27003761 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Entrectinib是一种口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制剂，IC50范围为 0.1~1.7 nM。Entrectinib (RXDX-101) 可诱导自噬。Phase 2。 | |||||
|---|---|---|---|---|---|---|
| 靶点 |
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| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05770544 | Recruiting | Solid Tumor|Haematological Malignancy|Malignancy|Malignant Neoplasm|Lymphoproliferative Disorders|Neoplasms by Histologic Type|Neoplasms by Site|Cancer|Brain Neoplasms|Melanoma|Glioma |
Cancer Research UK|University of Manchester|University of Birmingham|Royal Marsden NHS Foundation Trust|Hoffmann-La Roche |
December 2023 | Phase 2|Phase 3 |
| NCT04551495 | Recruiting | Invasive Lobular Breast Carcinoma|ER+ Breast Cancer|HER2-negative Breast Cancer |
Jules Bordet Institute|Hoffmann-La Roche |
January 14 2021 | Phase 2 |
| NCT04226833 | Completed | Hepatic Insufficiency |
Hoffmann-La Roche |
February 11 2020 | Phase 1 |
| NCT03796013 | Completed | Healthy Volunteers |
Genentech Inc. |
January 10 2019 | Phase 1 |
化学信息&溶解度
| 分子量 | 560.64 | 分子式 | C31H34F2N6O2 |
| CAS号 | 1108743-60-7 | SDF | Download Entrectinib SDF |
| Smiles | CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (178.36 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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