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Ro3280 PLK1 inhibitor,potent and highly selective

Catalog No.A8681
Size Price Stock Qty
10mM (in 1mL DMSO)
$251.00
In stock
5mg
$190.00
In stock
50mg
$980.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Ro3280

Biological Activity

Description RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with an IC50 value of 3 nM.
Targets PLK1          
IC50 3 nM          

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Chemical Properties

Cas No. 1062243-51-9 SDF Download SDF
Chemical Name 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Canonical SMILES CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC
Formula C27H35F2N7O3 M.Wt 543.61
Solubility >27.2mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Ro3280 is a selective inhibitor of PLK1 with IC50 value of 3 nM [1].

Polo-like kinase 1 (PLK1) is an enzyme and plays an important role in regulating cell cycles as an early trigger for G2/M phase transition. It has been shown that PLK1 is over-expressed in a variety of cancer cells and thus is regarded as a promising target for cancer drugs [2].

When tested with a panel of acute leukemia cell lines, Ro3280 showed inhibitory function on U937, HL 60, NB4, K562, MV4-11, and CCRF with IC50 value of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM, and 162 nM, respectively. It was interesting to notice that ALL cells (35.49-110.76 nM) were more sensitive to Ro3280 compared with AML cells (IC50, 52.80-147.50 nM). Further, it was showed that Ro3280 treatment decreased cell viability, induced apoptosis and disrupted cell cycle [3]. In H82 (lung cancer), HT-29 (colon cancer), MDA-MB-468 (breast cancer), PC3 (prostate cancer), and A375 (cutaneum carcinoma), Ro3280 treatment inhibited PLK1 with the IC50 was 5 nM, 10 nM, 19 nM, 12 nM, and 70 nM, respectively [1].

In nude mice model with HT-29 cells subcutaneous xenograft, administration of Ro3280 caused significant anti-tumor activity with 78% reduction at the dose of 40 mg/kg, once a week and then completely regressed tumor when more drug and more frequent [1].

References:
[1].  Chen, S., et al., Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett, 2012. 22(2): p. 1247-50.
[2].  Czaplinski, S., et al., Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis. Oncotarget, 2015.
[3].  Wang, N.N., et al., Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci, 2015. 16(1): p. 1266-92.