LXH254,LXH-254
LXH254,LXH-254 Basic information
- Product Name:
- LXH254,LXH-254
- Synonyms:
-
- LXH254; LXH-254; LXH 254
- LXH254,LXH-254
- LXH254
- 4-Pyridinecarboxamide, N-[3-[2-(2-hydroxyethoxy)-6-(4-morpholinyl)-4-pyridinyl]-4-methylphenyl]-2-(trifluoromethyl)-
- Naporafenib
- Bcr-Abl,A375,Inhibitor,p38 MAPK,LXH 254,inhibit,Raf,Mia PaCa-2,Raf kinases,HCT116,LXH254,Selective,MEL-JUSO,LXH-254
- N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide
- Naporafenib (LXH-254)
- CAS:
- 1800398-38-2
- MF:
- C25H25F3N4O4
- MW:
- 502.49
- Mol File:
- 1800398-38-2.mol
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LXH254,LXH-254 Chemical Properties
- Boiling point:
- 601.9±55.0 °C(Predicted)
- Density
- 1.353±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);199.0(Max Conc. mM)
- form
- A crystalline solid
- pka
- 10.86±0.70(Predicted)
- color
- Off-white to light yellow
- InChIKey
- UEPXBTCUIIGYCY-UHFFFAOYSA-N
- SMILES
- C1(C(F)(F)F)=NC=CC(C(NC2=CC=C(C)C(C3C=C(N4CCOCC4)N=C(OCCO)C=3)=C2)=O)=C1
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LXH254,LXH-254 Usage And Synthesis
Uses
LXH254, is a kinase inhibitor used in the treatment of solid tumors.
in vivo
Treatment with Naporafenib (Compound A) generates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C). Naporafenib exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes[1].
Naporafenib shows significant antitumor activity in models harboring BRAF mutations either alone or coincident with either activated NRAS or KRAS, and RAS mutants lacking ARAF are more sensitive to Naporafenib[2].
| Animal Model: | Outbred athymic (nu/nu) female mice and SCID Beige mice; BRAF-, NRAS-, and KRAS-mutant xenograft models, as well as a RAS/RAF wild-type model[2] |
| Dosage: | 100 mg/kg |
| Administration: | Orally, daily |
| Result: | Significantly decreased tumor volume in models harboring BRAF mutations either alone or coincident with either activated NRAS or KRAS, slightly decreased tumor volume in KRAS model. |
IC 50
CRAF: 0.072 nM (IC50); Braf: 0.21 nM (IC50); ARAF: 6.4 nM (IC50); p38α: 2.1 μM (IC50); Abl1: 4.9 μM (IC50)
LXH254,LXH-254Supplier
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