Name | PVM/MA |
Synonyms | E7386 E-7386 s-22611 PF06291874 Vorasidenib FM381 FM-381 6-(6-chloropyridin-2-yl)-N2,N4-bis((R)-1,1,1-trifluoropropan-2-yl)-1,3,5-triazine-2,4-diamine |
CAS | 1644545-52-7 |
Molecular Formula | C14H13ClF6N6 |
Molar Mass | 414.74 |
Density | 1.491±0.06 g/cm3(Predicted) |
Boling Point | 467.5±55.0 °C(Predicted) |
pKa | 1.49±0.41(Predicted) |
Storage Condition | 2-8℃ |
In vitro study | A pan-IDH1/2 inhibitor (AG881) selectively inhibits mutant IDH proteins and induces cell differentiation in in vitro and in vivo models. AG-881 inhibits the conversion of α-kg to cancer metabolite 2HG, inhibits 2HG-mediated signaling, and causes cell differentiation. Proliferation of tumor cells expressing mutant IDH is inhibited. |
In vivo study | AG-881 can completely cross the blood-brain barrier. At present, AG-881 is in the early clinical Phase I trial to detect its effect on the treatment of malignant hematological diseases, solid tumors and gliomas with IDH mutations. |
biological activity | Vorasidenib (AG-881) is an orally active inhibitor targeting mutant IDH1 and idh2. |
Target | Value |