LXH254,LXH-254
- Product Name
- LXH254,LXH-254
- CAS No.
- 1800398-38-2
- Chemical Name
- LXH254,LXH-254
- Synonyms
- LXH254;Naporafenib;LXH254,LXH-254;LXH254 (NAPORAFENIB);LXH254, 10 mM in DMSO;Naporafenib (LXH-254);LXH254; LXH-254; LXH 254;N-[3-[2-(2-Hydroxyethoxy)-6-morpholino-4-pyridyl]-4-methylphenyl]-2-(trifluoromethyl)isonicotinamide;N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide;N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide?, LXH254
- CBNumber
- CB23380035
- Molecular Formula
- C25H25F3N4O4
- Formula Weight
- 502.49
- MOL File
- 1800398-38-2.mol
LXH254,LXH-254 Property
- 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
Safety
- HS Code
- 2934999090
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 28231
- Product name
- LXH254
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 28231
- Product name
- LXH254
- Packaging
- 25mg
- Price
- $819
- Updated
- 2024/03/01
- Product number
- 28231
- Product name
- LXH254
- Packaging
- 5mg
- Price
- $270
- Updated
- 2024/03/01
- Product number
- 28231
- Product name
- LXH254
- Packaging
- 10mg
- Price
- $477
- Updated
- 2024/03/01
- Product number
- L395010
- Product name
- LXH254
- Packaging
- 25mg
- Price
- $1945
- Updated
- 2021/12/16
LXH254,LXH-254 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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