Naporafenib (LXH254)

Catalog No.S8745

For research use only.

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

CAS No. 1800398-38-2

Selleck's Naporafenib (LXH254) has been cited by 4 Publications

Purity & Quality Control

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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

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].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(199.0 mM)
Water Insoluble
Ethanol '34 mg/mL

Chemical Information

Molecular Weight 502.49
Formula

C25H25F3N4O4

CAS No. 1800398-38-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=NC=C2)C(F)(F)F)C3=CC(=NC(=C3)OCCO)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04417621 Recruiting Drug: LXH254|Drug: LTT462|Drug: Trametinib|Drug: Ribociclib Melanoma Novartis Pharmaceuticals|Novartis October 30 2020 Phase 2
NCT02974725 Recruiting Drug: LXH254|Drug: LTT462|Drug: Trametinib|Drug: Ribociclib Non-Small Cell Lung Cancer|Melanoma Novartis Pharmaceuticals|Novartis February 24 2017 Phase 1
NCT02607813 Active not recruiting Drug: LXH254|Drug: PDR001 NSCLC|Ovarian Cancer|Melanoma|Other Solid Tumors Novartis Pharmaceuticals|Novartis January 18 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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