[CAS NO. 1800398-38-2] Naporafenib (LXH254)
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PRODUCTS SPECIFICATIONS [1800398-38-2]
Store
Catalog
SLK-S8745
Brand
Selleck
CAS
1800398-38-2
DESCRIPTION [1800398-38-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 502.49 |
| Molecular Formula | C25H25F3N4O4 |
| SMILES | O=C(C1=CC(C(F)(F)F)=NC=C1)NC2=CC=C(C)C(C3=CC(OCCO)=NC(N4CCOCC4)=C3)=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9901 mL | 9.9504 mL | 19.9009 mL |
| 5 mM | 0.3980 mL | 1.9901 mL | 3.9802 mL |
| 10 mM | 0.1990 mL | 0.9950 mL | 1.9901 mL |
| 50 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL |
Description
Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
In vitro
LXH254 not only inhibits MAPK signaling activity in tumor models harboring BRAFV600 mutation, but also inhibits mutant N- and KRAS-driven signaling due to its ability to inhibit both RAF monomers and dimers with similar potencies. LXH254 is orally bioavailable, demonstrates a direct PK/PD relationship and causes tumor regression in multiple cell line and primary human tumor derived xenograft models at well-tolerated doses.
References
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