For research use only. Not for therapeutic Use.
Nirogacestat（Cat No.:I001124）is a potent, selective gamma-secretase inhibitor being developed for the treatment of desmoid tumors and other conditions driven by aberrant Notch signaling. By inhibiting gamma-secretase, Nirogacestat reduces tumor growth and fibrosis, offering a targeted approach to managing desmoid tumors, which are often difficult to treat with conventional therapies. Its efficacy and tolerability profile have demonstrated promise in clinical trials, positioning Nirogacestat as a potential therapeutic option for patients with these rare, aggressive tumors, improving outcomes and quality of life.
| Catalog Number | I001124 |
| CAS Number | 1290543-63-3 |
| Synonyms | PF-03084014 |
| Molecular Formula | C27H41F2N5O |
| Purity | 98% |
| Target | gamma-secretase |
| Target Protein | |
| Solubility | 10 mM in DMSO |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | 6.2 nM (γ-secretase) |
| IUPAC Name | (2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-N-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide |
| InChI | InChI=1S/C27H41F2N5O/c1-7-8-23(32-20-10-9-18-11-19(28)12-22(29)21(18)13-20)25(35)33-24-14-34(17-31-24)27(5,6)16-30-15-26(2,3)4/h11-12,14,17,20,23,30,32H,7-10,13,15-16H2,1-6H3,(H,33,35)/t20-,23-/m0/s1 |
| InChIKey | VFCRKLWBYMDAED-REWPJTCUSA-N |
| SMILES | CCC[C@@H](C(=O)NC1=CN(C=N1)C(C)(C)CNCC(C)(C)C)N[C@H]2CCC3=C(C2)C(=CC(=C3)F)F |
| Reference | </br>1:Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014. Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Wood DE, Wood KM, Van Deusen JW, Zhang L.Bioorg Med Chem Lett. 2011 May 1;21(9):2637-40. doi: 10.1016/j.bmcl.2010.12.118. Epub 2010 Dec 30. PMID: 21269827 </br>2:Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. Lanz TA, Wood KM, Richter KE, Nolan CE, Becker SL, Pozdnyakov N, Martin BA, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B.J Pharmacol Exp Ther. 2010 Jul;334(1):269-77. doi: 10.1124/jpet.110.167379. Epub 2010 Apr 2. PMID: 20363853 Free Article |
