1062169-56-5 Usage
Description
WYE-354 is a pyrazolopyrimidines derivative that serves as a potent and ATP-competitive mTOR inhibitor. It is characterized by its reduced activity against PI 3-Kα or PI 3-Kγ and is effective in blocking signaling through both mTOR complex 1 (mTORC1) and mTORC2. WYE-354 is a cell-permeable inhibitor with an IC50 of 4.3 nM, making it a valuable compound in the field of cancer research and treatment.
Uses
Used in Cancer Treatment:
WYE-354 is used as an mTOR inhibitor for its ability to effectively block cellular phosphorylation of S6K on T389 and Akt on S473. This leads to a significant suppression of tumor growth in various cancer types, including PC3MM2-derived tumors, where it demonstrated an 86% reduction in tumor growth on day 7 when administered at a dose of 50 mg/kg, i.p twice per day.
Used in Cell Cycle Regulation:
WYE-354 is used as a cell cycle regulator, inducing G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines. This property makes it a promising candidate for the development of cancer therapeutics, particularly for those resistant to traditional treatments.
Used in Preclinical Cancer Models:
WYE-354 is used as a research tool in preclinical cancer models to study its effects on tumor growth inhibition and to evaluate its potential as a therapeutic agent in nude mice with PTEN-null tumors. In these models, WYE-354 has demonstrated its ability to inhibit mTORC1 and mTORC2 in tumor-bearing mice, further supporting its potential as a cancer treatment option.
Used in Pharmaceutical Research:
WYE-354 is used as a research compound in the pharmaceutical industry for the development of new cancer treatments. Its potent inhibition of mTOR and selectivity over other kinases make it an attractive candidate for the design and synthesis of novel therapeutic agents targeting cancer cell growth and proliferation.
references
[1] qingsong liu, carson thoreen, jinhua wang, david sabatini, nathanael s. gray. mtor mediated anti-cancer drug discovery. drug discovery today. 2009. 6(2): 47-55.[2] shi-yong sun. mtor kinase inhibitors as potential cancer therapeutic drugs. cancer letters. 28 october 2013. 340(1): 1-8.
Check Digit Verification of cas no
The CAS Registry Mumber 1062169-56-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,6,2,1,6 and 9 respectively; the second part has 2 digits, 5 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1062169-56:
(9*1)+(8*0)+(7*6)+(6*2)+(5*1)+(4*6)+(3*9)+(2*5)+(1*6)=135
135 % 10 = 5
So 1062169-56-5 is a valid CAS Registry Number.
InChI:InChI=1S/C24H29N7O5/c1-34-23(32)26-17-5-3-16(4-6-17)20-27-21(29-11-13-36-14-12-29)19-15-25-31(22(19)28-20)18-7-9-30(10-8-18)24(33)35-2/h3-6,15,18H,7-14H2,1-2H3,(H,26,32)
1062169-56-5Relevant articles and documents
ATP-competitive inhibitors of the mammalian target of rapamycin: Design and synthesis of highly potent and selective pyrazolopyrimidines
Zask, Arie,Verheijen, Jeroen C.,Curran, Kevin,Kaplan, Joshua,Richard, David J.,Nowak, Pawel,Malwitz, David J.,Brooijmans, Natasja,Bard, Joel,Svenson, Kristine,Lucas, Judy,Toral-Barza, Lourdes,Zhang, Wei-Guo,Hollander, Irwin,Gibbons, James J.,Abraham, Robert T.,Ayral-Kaloustian, Semiramis,Mansour, Tarek S.,Yu, Ker
supporting information; experimental part, p. 5013 - 5016 (2010/03/04)
The mammalian target of rapamycin (mTOR), a central regulator of growth, survival, and metabolism, is a validated target for cancer therapy. Rapamycin and its analogues, allosteric inhibitors of mTOR, only partially inhibit one mTOR protein complex. ATP-competitive, global inhibitors of mTOR that have the potential for enhanced anticancer efficacy are described. Structural features leading to potency and selectivity were identified and refined leading to compounds with in vivo efficacy in tumor xenograft models.
