Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (2R)-2-[4-[4-(aminomethyl)-1,2-dihydro-1-oxo-6-phthalazinyl]-1-methyl-1H-pyrazol-5-yl]-4-chloro-6-(cyclopropyloxy)-3-fluoro-benzonitrile
Purity: ≥95%
Formula Markup: C23H18ClFN6O2
Formula Weight: 464.9
CAS Number: 2630904-45-7
Notes: MRTX-1719 is an inhibitor of the protein arginine methyltransferase 5 (PRMT5) and methylthioadenosine (MTA) complex.{67877} It selectively binds to the PRMT5/MTA complex over the PRMT5 and S-adenosyl-L-methionine (SAM) complex (Kds = 0.14 and 9.4 pM, respectively). MRTX-1719 selectively decreases protein dimethylarginine methylation levels in MTAP-/- HCT116 colon cancer cells, which lack methylthioadenosine phosphorylase (MTAP; IC50 = 8 nM), over wild-type HCT116 cells (IC50 = 653 nM), as well as selectively reduces the viability of MTAP-/- HCT116 cells (IC50 = 12 nM) over wild-type HCT116 cells (IC50 = 890 nM). In vivo, MRTX-1719 (12.5-100 mg/kg per day) reduces tumor volume in an MTAP-/- Lu-99 lung cancer mouse xenograft model.
Deutsch
English
