LXH254,LXH-254 manufacturers
- LXH254
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- $124.00
-
2026-08-30
- CAS:1800398-38-2
- Purity: 99.31%
- Supply Ability: 10g
- LXH254
-
- $124.00
-
2026-07-27
- CAS:1800398-38-2
- Purity: 99.31%
- Supply Ability: 10g
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| | 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)-;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);N-[3-[2-(2-Hydroxyethoxy)-6-morpholino-4-pyridyl]-4-methylphenyl]-2-(trifluoromethyl)isonicotinamide | | CAS: | 1800398-38-2 | | MF: | C25H25F3N4O4 | | MW: | 502.49 | | EINECS: | | | Product Categories: | | | Mol File: | 1800398-38-2.mol |  |
| | 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 |
| | 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-254 Preparation Products And Raw materials |
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