For research use only, not for therapeutic use.
ABT-869（Cat No.:I004909）is a potent multi-targeted tyrosine kinase inhibitor that primarily inhibits vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) signaling pathways. By blocking these receptors, ABT-869 disrupts angiogenesis and tumor growth, making it a valuable compound in cancer research. It is particularly effective in targeting solid tumors, such as those found in liver and kidney cancers, where abnormal angiogenesis plays a key role. ABT-869’s broad inhibition of kinases involved in tumor vasculature makes it a promising agent for developing anti-cancer therapies.
| Catalog Number | I004909 |
| CAS Number | 796967-16-3 |
| Synonyms | 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea |
| Molecular Formula | C₂₁H₁₈FN₅O |
| Purity | ≥95% |
| Target | VEGFR |
| Solubility | DMSO ≥72mg/mL Water <1.2mg/mL Ethanol ≥4.6mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 4 nM/3 nM/3 nM/4 nM /66 nM(KDR/CSF-1R/Flt-1/Flt-3PDGFRβ) |
| IUPAC Name | 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea |
| InChI | InChI=1S/C21H18FN5O/c1-12-5-10-16(22)18(11-12)25-21(28)24-14-8-6-13(7-9-14)15-3-2-4-17-19(15)20(23)27-26-17/h2-11H,1H3,(H3,23,26,27)(H2,24,25,28) |
| InChIKey | MPVGZUGXCQEXTM-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N |
| Reference | </br>1:Spectrophotometric and molecular modelling studies on in vitro interaction of tyrosine kinase inhibitor linifanib with bovine serum albumin. Wani TA, Bakheit AH, Zargar S, Hamidaddin MA, Darwish IA.PLoS One. 2017 Apr 18;12(4):e0176015. doi: 10.1371/journal.pone.0176015. eCollection 2017. PMID: 28419132 Free PMC Article</br>2:Micelle-enhanced direct spectrofluorimetric method for the determination of linifanib: Application to stability studies. Zawaneh AH, Khalil NN, Ibrahim SA, Al-Dafiri WN, Maher HM.Luminescence. 2017 Apr 5. doi: 10.1002/bio.3304. [Epub ahead of print] PMID: 28378538 </br>3:Phase II study of the Multikinase inhibitor of angiogenesis, Linifanib, in patients with metastatic and refractory colorectal cancer expressing mutated KRAS. Chan E, Goff LW, Cardin DB, Ancell K, Smith SJ, Whisenant JG, Ye F, Berlin JD.Invest New Drugs. 2017 Mar 28. doi: 10.1007/s10637-017-0458-8. [Epub ahead of print] PMID: 28353122 </br>4:Linifanib (ABT-869) Potentiates the Efficacy of Chemotherapeutic Agents through the Suppression of Receptor Tyrosine Kinase-Mediated AKT/mTOR Signaling Pathways in Gastric Cancer. Chen J, Guo J, Chen Z, Wang J, Liu M, Pang X.Sci Rep. 2016 Jul 8;6:29382. doi: 10.1038/srep29382. PMID: 27387652 Free PMC Article</br>5:Anti-vascular endothelial growth factor therapies at the crossroads: linifanib for non-small cell lung cancer. Horinouchi H.Transl Lung Cancer Res. 2016 Feb;5(1):78-81. doi: 10.3978/j.issn.2218-6751.2015.06.08. PMID: 26958495 Free PMC Article</br>6:Plasma biomarker signature associated with improved survival in advanced non-small cell lung cancer patients on linifanib. McKeegan EM, Ansell PJ, Davis G, Chan S, Chandran RK, Gawel SH, Dowell BL, Bhathena A, Chakravartty A, McKee MD, Ricker JL, Carlson DM, Ramalingam SS, Devanarayan V.Lung Cancer. 2015 Nov;90(2):296-301. doi: 10.1016/j.lungcan.2015.09.011. Epub 2015 Sep 15. PMID: 26424209 </br>7:Linifanib: current status and future potential in cancer therapy. Aversa C, Leone F, Zucchini G, Serini G, Geuna E, Milani A, Valdembri D, Martinello R, Montemurro F.Expert Rev Anticancer Ther. 2015 Jun;15(6):677-87. doi: 10.1586/14737140.2015.1042369. Epub 2015 May 2. Review. PMID: 25936222 </br>8:Linifanib–a multi-targeted receptor tyrosine kinase inhibitor and a low molecular weight gelator. Marlow M, Al-Ameedee M, Smith T, Wheeler S, Stocks MJ.Chem Commun (Camb). 2015 Apr 14;51(29):6384-7. doi: 10.1039/c5cc00454c. PMID: 25761611 </br>9:Randomized phase II study of carboplatin and paclitaxel with either linifanib or placebo for advanced nonsquamous non-small-cell lung cancer. Ramalingam SS, Shtivelband M, Soo RA, Barrios CH, Makhson A, Segalla JG, Pittman KB, Kolman P, Pereira JR, Srkalovic G, Belani CP, Axelrod R, Owonikoko TK, Qin Q, Qian J, McKeegan EM, Devanarayan V, McKee MD, Ricker JL, Carlson DM, Gorbunova VA.J Clin Oncol. 2015 Feb 10;33(5):433-41. doi: 10.1200/JCO.2014.55.7173. Epub 2015 Jan 5. PMID: 25559798 </br>10:Linifanib versus Sorafenib in patients with advanced hepatocellular carcinoma: results of a randomized phase III trial. Cainap C, Qin S, Huang WT, Chung IJ, Pan H, Cheng Y, Kudo M, Kang YK, Chen PJ, Toh HC, Gorbunova V, Eskens FA, Qian J, McKee MD, Ricker JL, Carlson DM, El-Nowiem S.J Clin Oncol. 2015 Jan 10;33(2):172-9. doi: 10.1200/JCO.2013.54.3298. Epub 2014 Dec 8. PMID: 25488963 Free PMC Article |
