1628805-46-8

Basic information

• Product Name: IDH-305
• Synonyms: IDH-305;(4R)-4-[(1S)-1-fluoroethyl]-3-(2-{[(1S)-1-[4-methyl-2'-(trifluoromethyl)-[3,4'-bipyridin]-6-yl]ethyl]amino}pyrimidin-4-yl)-1,3-oxazolidin-2-one
• CAS NO: 1628805-46-8
• Molecular Formula: C23H22F4N6O2
• Molecular Weight: 490.4533928
• EINECS: -0
• Mol File: 1628805-46-8.mol

Chemical Properties

• Boiling Point: 597.6±60.0 °C(Predicted)
• Appearance: /
• Density: 1.370±0.06 g/cm3(Predicted)
• PKA: 4.07±0.10(Predicted)
• CAS DataBase Reference: IDH-305(CAS DataBase Reference)
• NIST Chemistry Reference: IDH-305(1628805-46-8)
• EPA Substance Registry System: IDH-305(1628805-46-8)

Safety Data

• Hazardous Substances Data: 1628805-46-8(Hazardous Substances Data)

Usage

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.

Upstream product

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Relevant articles and documents

Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor

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.

3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH

The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.