1062243-51-9 Usage
Description
RO3280, a Polo-like kinase 1 (PLK1) inhibitor, is a potent compound that has demonstrated significant antitumor activity in xenograft mouse models. It is characterized by its good selectivity against other kinases and excellent in vitro cellular potency, making it a promising candidate for cancer treatment.
Uses
Used in Anticancer Applications:
RO3280 is used as an anticancer agent for its strong antitumor activity in xenograft mouse models. It targets Polo-like kinase 1 (PLK1), a key enzyme involved in cell division and proliferation, thereby inhibiting the growth and progression of cancer cells.
Used in Drug Development:
RO3280 is used as a lead compound in the development of novel cancer therapeutics due to its good selectivity against other kinases and excellent in vitro cellular potency. This makes it a valuable starting point for designing and optimizing new drugs with improved efficacy and reduced side effects.
Used in Cancer Research:
RO3280 is used as a research tool for studying the role of PLK1 in cancer cell division and proliferation. Its potent inhibitory effects on PLK1 make it an ideal candidate for investigating the underlying mechanisms of cancer development and identifying potential therapeutic targets.
Used in Pharmaceutical Industry:
RO3280 is used as a key component in the development of targeted cancer therapies within the pharmaceutical industry. Its strong antitumor activity and selectivity for PLK1 make it a valuable asset in the ongoing efforts to create more effective and personalized cancer treatments.
Biological Activity
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1062243-51-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,6,2,2,4 and 3 respectively; the second part has 2 digits, 5 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1062243-51:
(9*1)+(8*0)+(7*6)+(6*2)+(5*2)+(4*4)+(3*3)+(2*5)+(1*1)=109
109 % 10 = 9
So 1062243-51-9 is a valid CAS Registry Number.
1062243-51-9Relevant articles and documents
Identification of novel, potent and selective inhibitors of Polo-like kinase 1
Chen, Shaoqing,Bartkovitz, David,Cai, Jianping,Chen, Yi,Chen, Zhi,Chu, Xin-Jie,Le, Kang,Le, Nam T.,Luk, Kin-Chun,Mischke, Steve,Naderi-Oboodi, Goli,Boylan, John F.,Nevins, Tom,Qing, Weiguo,Chen, Yingsi,Wovkulich, Peter M.
, p. 1247 - 1250 (2012/03/26)
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 excell
HALO-SUBSTITUTED PYRIMIDODIAZEPINES
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Page/Page column 32, (2009/12/28)
The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
