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My CartCAS：1108743-60-7
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to light yellow Solid
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| CAS | 1108743-60-7 |
| Name | Entrectinib |
| Molecular Formula | C31H34F2N6O2 |
| Molecular Weight | 560.64 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | Off-white to light yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28129099 |
| SMILES | CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6 |
| InChIKey | HAYYBYPASCDWEQ-UHFFFAOYSA-N |
| InChI | InChI=1S/C31H34F2N6O2/c1-38-8-10-39(11-9-38)25-3-4-26(29(19-25)34-24-6-12-41-13-7-24)31(40)35-30-27-17-20(2-5-28(27)36-37-30)14-21-15-22(32)18-23(33)16-21/h2-5，15-19，24，34H，6-14H2，1H3，(H2，35，36，37，40) |
| PubChem CID | 25141092 |
| Target Point | ROS Kinase;Trk Receptor;Anaplastic lymphoma kinase (ALK) |
| Passage | Protein Tyrosine Kinase/RTK;Neuronal Signaling;Angiogenesis |
| Background | It is a potent, orally active and central neuroactive inhibitor of Trk, ROS1 and ALK. |
| Biological Activity | Entrectinib是一种具有口服活性、BBB穿透性和中心活性的TrkA/B/C、ROS1和ALK抑制剂，其IC50值分别为1、3、5、12和7 nM。能诱导癌细胞凋亡和周期停滞，具有抗肿瘤活性，并能减轻博莱霉素诱导的小鼠肺纤维化。[1-3] |
| IC50 | TrkA: 1nM(IC50);TrkB: 3nM(IC50);ROS1: 12nM(IC50);ALK: 7nM(IC50)[1] |
| In Vitro | 针对 200 多种人类肿瘤细胞系进行的增殖分析表明，恩曲替尼在体外对依赖该药物药理靶点的细胞系具有极强的抑制作用[1]。恩曲替尼能剂量依赖性地抑制TGF-β1/non-Smad信号传导，减轻TGF-β1诱导的成纤维细胞活化和上皮-间质转化(EMT)[2]。恩替瑞尼能明显抑制体外表达TrkB的NB细胞的生长，与Irino-TMZ联用时，它能明显增强Irino-TMZ的生长抑制作用[3]。 |
| In Vivo | 肿瘤小鼠口服恩曲替尼能诱导相关的人类异种移植肿瘤消退，包括依赖 TRKA 的结直肠癌 KM12、ROS1 驱动的肿瘤和几种不同组织来源的 ALK 依赖性模型，包括脑定位肺癌转移模型[1]。恩曲替尼能有效缓解博莱霉素诱导的小鼠肺纤维化[2]。 |
| Data Literature Source | [1]. Ardini E，et al. Entrectinib，a Pan-TRK，ROS1，and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications. Mol Cancer Ther. 2016 Apr;15(4): 628-39. [2]. Miao Y，et al. Entrectinib ameliorates bleomycin-induced pulmonary fibrosis in mice by inhibiting TGF-β1 signaling pathway. Int Immunopharmacol. 2022 Dec;113(Pt B): 109427. [3]. Iyer R，et al. Entrectinib is a potent inhibitor of Trk-driven neuroblastomas in a xenograft mouse model. Cancer Lett. 2016 Mar 28;372(2): 179-86. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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