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SML2038

Sigma-Aldrich

RO3280

≥98% (HPLC)

Synonym(s):

4-[(9-Cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide, Ro 3280, Ro3280

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About This Item

Empirical Formula (Hill Notation):
C27H35F2N7O3
CAS Number:
1062243-51-9
Molecular Weight:
543.61
MDL number:
MFCD22665717
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

FC1(F)CN(C2CCCC2)C3=NC(NC4=CC=C(C(NC5CCN(C)CC5)=O)C=C4OC)=NC=C3N(C)C1=O

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)

InChI key

DJNZZLZKAXGMMC-UHFFFAOYSA-N

Biochem/physiol Actions

RO3280 is a potent and selective Polo-like kinase 1 (PLK1) inhibitor. RO3280 induces mitotic catastrophe and apoptosis in human bladder cancer cells and leukemia cells.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Shaoqing Chen et al.
Bioorganic & medicinal chemistry letters, 22(2), 1247-1250 (2011-12-17)
A series of pyrimidodiazepines was identified as potent Polo-like kinase 1 (PLK1) inhibitors. The synthesis and SAR are discussed. The lead compound 7 (RO3280) has potent inhibitory activity against PLK1, good selectivity against other kinases, and excellent in vitro cellular
Zhe Zhang et al.
Journal of cellular and molecular medicine, 21(4), 758-767 (2016-11-24)
Bladder cancer is a common cancer with particularly high recurrence after transurethral resection. Despite improvements in neoadjuvant chemotherapy, the outcome of patients with advanced bladder cancer has changed very little. In this study, the anti-tumour activities of a novel Polo-like
Circannual rhythm in response of renin release to calcium deprivation in isolated rat glomeruli.
B Wu et al.
Progress in clinical and biological research, 341A, 511-516 (1990-01-01)
Na-Na Wang et al.
International journal of molecular sciences, 16(1), 1266-1292 (2015-01-13)
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. RO3280 was recently identified as a novel PLK1 inhibitor; however its therapeutic effects

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