Home MAPK Raf inhibitor Naporafenib (LXH254) For research use only.

Naporafenib (LXH254)

Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.

Naporafenib (LXH254) Chemical Structure

Naporafenib (LXH254) Chemical Structure

CAS No. 1800398-38-2

Purity & Quality Control

Naporafenib (LXH254) Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Biological Activity

Description Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
Targets
B-Raf [1] C-Raf [1]
In vitro
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[1].
Cell Research Cell lines Ku-19-19 cells
Concentrations 2 μM
Incubation Time 3 days
Method

For crystal violet staining experiments, cells were seeded in 6-well plates at 50,000 to 100,000 cells/well for 3-day experiments and vehicle or drug (diluted in media) was added the day after plating.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04417621 Active not recruiting
Melanoma
Novartis Pharmaceuticals|Novartis
 October 30 2020 Phase 2
NCT02974725 Active not recruiting
Non-Small Cell Lung Cancer|Melanoma
Novartis Pharmaceuticals|Novartis
 February 24 2017 Phase 1
NCT02607813 Terminated
NSCLC|Ovarian Cancer|Melanoma|Other Solid Tumors
Novartis Pharmaceuticals|Novartis
 January 18 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 502.49 Formula

C25H25F3N4O4
CAS No. 1800398-38-2 SDF --
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=NC=C2)C(F)(F)F)C3=CC(=NC(=C3)OCCO)N4CCOCC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (199.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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