1454682-72-4 Usage
Uses
Used in Oncology:
LY-3009120 is used as an anticancer agent for the inhibition of tumors. Its dose-dependent inhibition property allows for precise control over the level of Rad protein inhibition, which can be tailored to the specific needs of each patient and type of cancer. By targeting and inhibiting the Rad proteins, LY-3009120 can effectively disrupt the DNA repair process in cancer cells, leading to the prevention of tumor growth and the promotion of cancer cell death. This makes it a promising candidate for the treatment of various types of cancer.
Biological Activity
ly3009120 is a pan-raf and raf dimer inhibitor. it inhibits braf wt, craf, wt, brafv600e, and brafv600e+g468a with the ic50 values of 9.1, 15, 5.8, and 17 nm, respectively. [1]raf is family of serine/threonine-protein kinase mediates ras gtpases and the mapk/erk cascade. it involves in proliferation, differentiation, apoptosis, survival and oncogenic transformation. [1]in nras mutant sk-mel2 cells or kras mutant hct116 cells, ly3009120 inhibits the kinase activity of craf in a dose-dependent manner and induces braf/craf heterodimerization. it also blocks phospho-mek and -erk and induces minimal paradoxical activation in ras mutant cells. moreover, treatment of braf v600e a375 melanoma cells by ly3009120 for 24 hr predominantly induces a g0/g1 arrest with more than 95% cells in g0/g1 phase. [1]in nude rats bearing a375 xenograft tumors, oral ly3001920 treatment exerts a dose-dependent inhibition of phospho-mek and –erk. 15 or 30 mg/kg ly3009120 shows near complete tumor regression in nude rats bearing pdx tumors. [1]
references
1. peng sb, henry jr, kaufman md et al. inhibition of raf isoforms and active dimers by ly3009120 leads to anti-tumor activities in ras or braf mutant cancers. cancer cell. 2015 sep 14;28(3):384-98.
Check Digit Verification of cas no
The CAS Registry Mumber 1454682-72-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,5,4,6,8 and 2 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1454682-72:
(9*1)+(8*4)+(7*5)+(6*4)+(5*6)+(4*8)+(3*2)+(2*7)+(1*2)=184
184 % 10 = 4
So 1454682-72-4 is a valid CAS Registry Number.
1454682-72-4Relevant articles and documents
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3- d ]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells
Henry, James R.,Kaufman, Michael D.,Peng, Sheng-Bin,Ahn, Yu Mi,Caldwell, Timothy M.,Vogeti, Lakshminarayana,Telikepalli, Hanumaiah,Lu, Wei-Ping,Hood, Molly M.,Rutkoski, Thomas J.,Smith, Bryan D.,Vogeti, Subha,Miller, David,Wise, Scott C.,Chun, Lawrence,Zhang, Xiaoyi,Zhang, Youyan,Kays, Lisa,Hipskind, Philip A.,Wrobleski, Aaron D.,Lobb, Karen L.,Clay, Julia M.,Cohen, Jeffrey D.,Walgren, Jennie L.,McCann, Denis,Patel, Phenil,Clawson, David K.,Guo, Sherry,Manglicmot, Danalyn,Groshong, Chris,Logan, Cheyenne,Starling, James J.,Flynn, Daniel L.
, p. 4165 - 4179 (2015/06/08)
The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clinical efficac
2-AMINO, 6-PHENYL SUBSTITUTED PYRIDO [2, 3 - D] PYRIMIDINE DERIVATIVES USEFUL AS RAF KINASE INHIBITORS
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, (2013/09/26)
The present invention provides the compound l-(3,3-Dimethylbutyl) -3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in tr
