AMG-900

• CAT Number: I005627
• CAS Number: 945595-80-2
• Molecular Formula: C₂₈H₂₁N₇OS
• Molecular Weight: 503.58
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: DMSO ≥95mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20℃ powder
• IC50: 5 nM(Aurora A); 4 nM(Aurora B); 1 nM(Aurora C)
• IUPAC Name: N-[4-[3-(2-aminopyrimidin-4-yl)pyridin-2-yl]oxyphenyl]-4-(4-methylthiophen-2-yl)phthalazin-1-amine
• InChI: 1S/C28H21N7OS/c1-17-15-24(37-16-17)25-20-5-2-3-6-21(20)26(35-34-25)32-18-8-10-19(11-9-18)36-27-22(7-4-13-30-27)23-12-14-31-28(29)33-23/h2-16H,1H3,(H,32,35(H2,29,31,33)
• InChIKey: IVUGFMLRJOCGAS-UHFFFAOYSA-N
• SMILES: CC1=CSC(=C1)C2=NN=C(C3=CC=CC=C32)NC4=CC=C(C=C4)OC5=C(C=CC=N5)C6=NC(=NC=C6)N

AMG-900 (Cat.No:I005627) is a potent and selective inhibitor of aurora kinase A/B, a group of serine/threonine kinases involved in cell cycle regulation. It has shown promising anticancer activity in preclinical studies and is currently being investigated in clinical trials for the treatment of various solid tumors and hematologic malignancies. 

Reference

1:The aurora kinase inhibitor AMG 900 increases apoptosis and induces chemosensitivity to anticancer drugs in the NCI-H295 adrenocortical carcinoma cell line. Borges KS, Andrade AF, Silveira VS, Marco Antonio DS, Vasconcelos EJR, Antonini SRR, Tone LG, Scrideli CA.Anticancer Drugs. 2017 Jul;28(6):634-644. doi: 10.1097/CAD.0000000000000504. PMID: 28410270 2:A Phase 1 Study of AMG 900, an Orally Administered Pan-Aurora Kinase Inhibitor, in Adult Patients With Acute Myeloid Leukemia. Kantarjian HM, Schuster MW, Jain N, Advani A, Jabbour E, Gamelin E, Rasmussen E, Juan G, Anderson A, Chow VF, Friberg G, Vogl FD, Sekeres MA.Am J Hematol. 2017 Mar 28. doi: 10.1002/ajh.24736. [Epub ahead of print] PMID: 28370201 3:Antitumour activity of AMG 900 alone or in combination with histone deacetylase inhibitor SaHa on medulloblastoma cell lines. Geron L, Borges KS, Andrade AF, Suazo VK, Scrideli CA, Tone LG.Neurol Res. 2015 Aug;37(8):703-11. doi: 10.1179/1743132815Y.0000000048. Epub 2015 May 22. PMID: 26000978 4:Discovery of N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), a highly selective, orally bioavailable inhibitor of aurora kinases with activity against multidrug-resistant cancer cell lines. Geuns-Meyer S, Cee VJ, Deak HL, Du B, Hodous BL, Nguyen HN, Olivieri PR, Schenkel LB, Vaida KR, Andrews P, Bak A, Be X, Beltran PJ, Bush TL, Chaves MK, Chung G, Dai Y, Eden P, Hanestad K, Huang L, Lin MH, Tang J, Ziegler B, Radinsky R, Kendall R, Patel VF, Payton M.J Med Chem. 2015 Jul 9;58(13):5189-207. doi: 10.1021/acs.jmedchem.5b00183. Epub 2015 May 31. PMID: 25970324 5:AMG 900, a potent inhibitor of aurora kinases causes pharmacodynamic changes in p-Histone H3 immunoreactivity in human tumor xenografts and proliferating mouse tissues. Juan G, Bush TL, Ma C, Manoukian R, Chung G, Hawkins JM, Zoog S, Kendall R, Radinsky R, Loberg R, Friberg G, Payton M.J Transl Med. 2014 Nov 4;12:307. doi: 10.1186/s12967-014-0307-x. PMID: 25367255 Free PMC Article6:Combining the pan-aurora kinase inhibitor AMG 900 with histone deacetylase inhibitors enhances antitumor activity in prostate cancer. Paller CJ, Wissing MD, Mendonca J, Sharma A, Kim E, Kim HS, Kortenhorst MS, Gerber S, Rosen M, Shaikh F, Zahurak ML, Rudek MA, Hammers H, Rudin CM, Carducci MA, Kachhap SK.Cancer Med. 2014 Oct;3(5):1322-35. doi: 10.1002/cam4.289. Epub 2014 Jul 3. PMID: 24989836 Free PMC Article7:AMG 900, pan-Aurora kinase inhibitor, preferentially inhibits the proliferation of breast cancer cell lines with dysfunctional p53. Kalous O, Conklin D, Desai AJ, Dering J, Goldstein J, Ginther C, Anderson L, Lu M, Kolarova T, Eckardt MA, Langerød A, Børresen-Dale AL, Slamon DJ, Finn RS.Breast Cancer Res Treat. 2013 Oct;141(3):397-408. doi: 10.1007/s10549-013-2702-z. Epub 2013 Oct 5. PMID: 24091768 8:AMG 900, a small-molecule inhibitor of aurora kinases, potentiates the activity of microtubule-targeting agents in human metastatic breast cancer models. Bush TL, Payton M, Heller S, Chung G, Hanestad K, Rottman JB, Loberg R, Friberg G, Kendall RL, Saffran D, Radinsky R.Mol Cancer Ther. 2013 Nov;12(11):2356-66. doi: 10.1158/1535-7163.MCT-12-1178. Epub 2013 Aug 29. PMID: 23990115 Free Article9:LC-MS/MS bioanalytical method development for AMG 900: resolution of an isobaric interference in rodent in vivo studies. Be X, Moore ES, Zhao Z, Wells MC.J Pharm Biomed Anal. 2013 Feb 23;74:171-7. doi: 10.1016/j.jpba.2012.10.026. Epub 2012 Nov 2. PMID: 23245248 10:Gender effects on rat metabolism of AMG 900, an orally available small molecule aurora kinase inhibitor. Waldon D, Berry L, Lin MH, Schenkel L, Hollis LS, Zhao Z.Drug Metab Lett. 2011 Dec;5(4):290-7. PMID: 22022868