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LXH254
- Naporafenib
- Soluble in DMSO and EtOH
- MF: C25H25F3N4O4
- MW: 502.49
Description
LXH254 is a potent, selective, orally available and ARAF-sparing type II inhibitor of BRAF and CRAF with IC50 values of 0.21 and 0.072 mM for BRAF and CRAF, respectively.
More Information
| Parent CAS No. | 1800398-38-2 |
|---|---|
| Chemical Name | N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide |
| SMILES | O1CCN(C2C=C(C3C(C)=CC=C(NC(=O)C4C=CN=C(C(F)(F)F)C=4)C=3)C=C(OCCO)N=2)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H25F3N4O4/c1-16-2-3-19(30-24(34)17-4-5-29-21(12-17)25(26,27)28)15-20(16)18-13-22(32-6-9-35-10-7-32)31-23(14-18)36-11-8-33/h2-5,12-15,33H,6-11H2,1H3,(H,30,34) |
| InChiKey | UEPXBTCUIIGYCY-UHFFFAOYSA-N |
| CID | 90456533 |
| Short Description | B/C RAF inhibitor |
References
- S Ramurthy et al. Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic. J Med Chem. 2020 Mar 12;63(5):2013-2027.
- KA Monaco et al. LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors. Clin Cancer Res. 2021 Apr 1;27(7):2061-2073.
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