1628805-46-8 Usage
Description
IDH-305, also known as (4R)-4-[(1S)-1-Fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-2''-(trifluoromethyl)[3,4''-bipyridin]-6-yl]ethyl]amino]-4-pyrimidinyl]-2-oxazolidinone, is an inhibitor of isocitrate dehydrogenase (IDH), an essential enzyme for cellular respiration in the tricarboxylic acid (TCA) cycle. It plays a crucial role in regulating cellular metabolism and has been identified as a potential therapeutic target for various diseases.
Uses
Used in Pharmaceutical Industry:
IDH-305 is used as an inhibitor for isocitrate dehydrogenase (IDH) for its potential therapeutic applications in treating diseases associated with the dysregulation of cellular metabolism. By targeting the IDH enzyme, IDH-305 can help regulate cellular respiration and potentially offer treatment options for conditions related to metabolic imbalances.
Used in Oncology:
IDH-305 is used as an anticancer agent, particularly in the treatment of tumors with IDH mutations. It works by inhibiting the mutated IDH enzyme, which can lead to the accumulation of oncometabolites and contribute to the development and progression of cancer. By blocking this enzyme, IDH-305 may help prevent the formation of these harmful metabolites and slow down tumor growth.
Used in Drug Development:
IDH-305 is used as a lead compound in the development of new drugs targeting IDH enzymes. Its structure and mechanism of action provide valuable insights for the design of more potent and selective inhibitors, which could be used in combination therapies or as standalone treatments for various diseases.
Used in Research:
IDH-305 is used as a research tool to study the role of IDH enzymes in cellular metabolism and disease progression. It can help researchers understand the molecular mechanisms underlying IDH-related diseases and identify potential therapeutic targets for drug development.
Check Digit Verification of cas no
The CAS Registry Mumber 1628805-46-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,6,2,8,8,0 and 5 respectively; the second part has 2 digits, 4 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1628805-46:
(9*1)+(8*6)+(7*2)+(6*8)+(5*8)+(4*0)+(3*5)+(2*4)+(1*6)=188
188 % 10 = 8
So 1628805-46-8 is a valid CAS Registry Number.
1628805-46-8Relevant articles and documents
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor
Cho, Young Shin,Levell, Julian R.,Liu, Gang,Caferro, Thomas,Sutton, James,Shafer, Cynthia M.,Costales, Abran,Manning, James R.,Zhao, Qian,Sendzik, Martin,Shultz, Michael,Chenail, Gregg,Dooley, Julia,Villalba, Brian,Farsidjani, Ali,Chen, Jinyun,Kulathila, Raviraj,Xie, Xiaoling,Dodd, Stephanie,Gould, Ty,Liang, Guiqing,Heimbach, Tycho,Slocum, Kelly,Firestone, Brant,Pu, Minying,Pagliarini, Raymond,Growney, Joseph D.
, p. 1116 - 1121 (2017/10/18)
Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg132. Having identified an allosteric, induced pocket of IDH1R132H, we have explored 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant IDH1 inhibitors for in vivo modulation of 2-HG production and potential brain penetration. We report here optimization efforts toward the identification of clinical candidate IDH305 (13), a potent and selective mutant IDH1 inhibitor that has demonstrated brain exposure in rodents. Preclinical characterization of this compound exhibited in vivo correlation of 2-HG reduction and efficacy in a patient-derived IDH1 mutant xenograft tumor model. IDH305 (13) has progressed into human clinical trials for the treatment of cancers with IDH1 mutation.
