WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406354
Description: RO3280, also known as Ro5203280, is a potent and selective PLK 1 inhibitor with excellent in vitro cellular potency. RO3280 showed strong antitumor activity in xenograft mouse models. he 50% inhibitory concentration (IC50) of RO3280 for acute leukemia cells was between 74 and 797 nM. The IC50 of RO3280 in primary acute lymphocytic leukemia (ALL) and AML cells was between 35.49 and 110.76 nM and 52.80 and 147.50 nM, respectively. RO3280 induced apoptosis and cell cycle disorder in leukemia cells. RO3280 treatment regulated several apoptosis-associated genes. Polo-like kinase 1 (PLK1) is highly expressed in many cancers and therefore a biomarker of transformation and potential target for the development of cancer-specific small molecule drugs.
MedKoo Cat#: 406354
Chemical Formula: C27H35F2N7O3
Exact Mass: 543.27694
Molecular Weight: 543.61
Elemental Analysis: C, 59.65; H, 6.49; F, 6.99; N, 18.04; O, 8.83
Synonym: RO3280; RO-3280; RO 3280; Ro5203280; Ro-5203280; Ro 5203280.
IUPAC/Chemical Name: 4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
InChi Key: DJNZZLZKAXGMMC-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H35F2N7O3/c1-34-12-10-18(11-13-34)31-24(37)17-8-9-20(22(14-17)39-3)32-26-30-15-21-23(33-26)36(19-6-4-5-7-19)16-27(28,29)25(38)35(21)2/h8-9,14-15,18-19H,4-7,10-13,16H2,1-3H3,(H,31,37)(H,30,32,33)
SMILES Code: O=C(NC1CCN(C)CC1)C2=CC=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C(OC)=C2
1: Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S, Naderi-Oboodi G, Boylan JF, Nevins T, Qing W, Chen Y, Wovkulich PM. Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50. doi: 10.1016/j.bmcl.2011.11.052. Epub 2011 Dec 1. PubMed PMID: 22172702.