Home MAPK Raf inhibitor Naporafenib (LXH254)

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Naporafenib (LXH254) Raf inhibitor

Cat.No.S8745

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

Chemical Structure

Molecular Weight: 502.49

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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (199.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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Chemical Information, Storage & Stability

Molecular Weight 502.49 Formula

C25H25F3N4O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1800398-38-2 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=NC=C2)C(F)(F)F)C3=CC(=NC(=C3)OCCO)N4CCOCC4

Mechanism of Action

Targets/IC50/Ki
B-Raf
C-Raf
In vitro

Naporafenib (LXH254) not only inhibits MAPK signaling activity in tumor models harboring BRAFV600 mutation, but also suppresses mutant N- and KRAS-driven signaling due to its ability to inhibit both RAF monomers and dimers with similar potencies. It 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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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