2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Mutant IDH1 · Literature evidence
Biological Activity
IDH-305 (IDH305) is an allosteric mutant-IDH1 inhibitor for studies of 2-hydroxyglutarate production and IDH1-mutant cancer biology. IDH305 was identified as compound 13, targeting mutant-IDH1-dependent 2-hydroxyglutarate production.
IDH305 was identified as compound 13, targeting mutant-IDH1-dependent 2-hydroxyglutarate production.
In Vivo
Endpoint
Model / conditions / source
Reported result
Brain exposure
Rodent pharmacokinetic evaluation. [1], abstract
Brain exposure was demonstrated; the verified abstract does not provide a brain-to-plasma ratio or full dose schedule.
Pharmacodynamic efficacy
Patient-derived IDH1-mutant tumor xenograft. [1]
Reduction in 2-hydroxyglutarate correlated with antitumor efficacy.
Compound and Evidence Context
Endpoint
Model / conditions / source
Reported result
Applicability
Mutant-IDH1 preclinical evidence. [1]
The findings are mutation- and model-specific. An exact biochemical IC50 or brain exposure value is not supplied without verification of the corresponding table.
Interpretation
Brain exposure and xenograft response are distinct endpoints; neither alone establishes clinical brain-tumor efficacy.
NCT-503 is a PHGDH inhibitor for studying serine synthesis, one-carbon metabolism and metabolic dependencies in cancer models. Published studies distinguish biochemical inhibition from cellular growth effects and document context-dependent off-target activity.
