For research use only. Not for therapeutic Use.
TAK-285（Cat No.:I005244）is a selective small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is involved in the regulation of cell growth and survival. By inhibiting EGFR signaling, TAK-285 aims to block tumor cell proliferation and induce cell death, making it a potential treatment for cancers, particularly those with EGFR overexpression or mutations, such as non-small cell lung cancer (NSCLC) and colorectal cancer. Preclinical studies have demonstrated its anti-tumor activity, though further clinical trials are needed to evaluate its safety, pharmacokinetics, and therapeutic potential in human cancer treatment.
| Catalog Number | I005244 |
| CAS Number | 871026-44-7 |
| Synonyms | N-[2-[4-[3-chloro-4-[3-(trifluoromethyl)phenoxy]anilino]pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide |
| Molecular Formula | C26H25ClF3N5O3 |
| Purity | ≥95% |
| Target | Protein Tyrosine Kinase/RTK |
| Solubility | DMSO 110 mg/ml |
| Storage | 3 years -20C powder |
| IC50 | 17/23 nM (HER2/1) |
| IUPAC Name | N-[2-[4-[3-chloro-4-[3-(trifluoromethyl)phenoxy]anilino]pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide |
| InChI | InChI=1S/C26H25ClF3N5O3/c1-25(2,37)14-22(36)31-9-11-35-10-8-20-23(35)24(33-15-32-20)34-17-6-7-21(19(27)13-17)38-18-5-3-4-16(12-18)26(28,29)30/h3-8,10,12-13,15,37H,9,11,14H2,1-2H3,(H,31,36)(H,32,33,34) |
| InChIKey | ZYQXEVJIFYIBHZ-UHFFFAOYSA-N |
| SMILES | CC(C)(CC(=O)NCCN1C=CC2=C1C(=NC=N2)NC3=CC(=C(C=C3)OC4=CC=CC(=C4)C(F)(F)F)Cl)O |
| Reference | </br>1:HER2 and HER3 cooperatively regulate cancer cell growth and determine sensitivity to the novel investigational EGFR/HER2 kinase inhibitor TAK-285. Takagi S, Banno H, Hayashi A, Tamura T, Ishikawa T, Ohta Y.Oncoscience. 2014 Mar 24;1(3):196-204. eCollection 2014. PMID: 25594012 Free PMC Article</br>2:Antitumor Activity of TAK-285, an Investigational, Non-Pgp Substrate HER2/EGFR Kinase Inhibitor, in Cultured Tumor Cells, Mouse and Rat Xenograft Tumors, and in an HER2-Positive Brain Metastasis Model. Nakayama A, Takagi S, Yusa T, Yaguchi M, Hayashi A, Tamura T, Kawakita Y, Ishikawa T, Ohta Y.J Cancer. 2013 Aug 16;4(7):557-65. doi: 10.7150/jca.6689. eCollection 2013. PMID: 23983820 Free PMC Article</br>3:Phase 1 dose-escalation, pharmacokinetic, and cerebrospinal fluid distribution study of TAK-285, an investigational inhibitor of EGFR and HER2. LoRusso P, Venkatakrishnan K, Chiorean EG, Noe D, Wu JT, Sankoh S, Corvez M, Sausville EA.Invest New Drugs. 2014 Feb;32(1):160-70. doi: 10.1007/s10637-013-9988-x. Epub 2013 Jul 2. PMID: 23817974 Free PMC Article</br>4:Verification of brain penetration of the unbound fraction of a novel HER2/EGFR dual kinase inhibitor (TAK-285) by microdialysis in rats. Erdo F, Gordon J, Wu JT, Sziráki I.Brain Res Bull. 2012 Mar 10;87(4-5):413-9. doi: 10.1016/j.brainresbull.2012.01.002. Epub 2012 Jan 9. PMID: 22245027 </br>5:Phase I first-in-human study of TAK-285, a novel investigational dual HER2/EGFR inhibitor, in cancer patients. Doi T, Takiuchi H, Ohtsu A, Fuse N, Goto M, Yoshida M, Dote N, Kuze Y, Jinno F, Fujimoto M, Takubo T, Nakayama N, Tsutsumi R.Br J Cancer. 2012 Feb 14;106(4):666-72. doi: 10.1038/bjc.2011.590. Epub 2012 Jan 12. PMID: 22240796 Free PMC Article |
