Home Cytoskeletal Signaling PKC inhibitor Darovasertib (LXS-196) For research use only.

Darovasertib (LXS-196)

Synonyms: IDE-196

Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).

Darovasertib (LXS-196) Chemical Structure

Darovasertib (LXS-196) Chemical Structure

CAS No. 1874276-76-2

Purity & Quality Control

Darovasertib (LXS-196) Related Products

Signaling Pathway

PKC Signaling Pathways

PKC Signaling Pathway

Biological Activity

Description Darovasertib (LXS-196, IDE-196) is a selective inhibitor of protein kinase C (PKC).
Targets
PKC [1]
In vitro
In vitro

LXS-196 (Darovasertib) is a highly specific PKC inhibitor that resulted in a concentration dependent inhibition of immunoprecipitated LRRK1 kinase activity, with an IC50 of ∼40 nM.
Cell Research Cell lines HEK293 cells
Concentrations ∼40 nM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of the drug for 24 hour.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05907954 Recruiting
Uveal Melanoma
IDEAYA Biosciences
 July 3 2023 Phase 2
NCT03947385 Recruiting
Metastatic Uveal Melanoma|Cutaneous Melanoma|Colorectal Cancer|Other Solid Tumors
IDEAYA Biosciences
 June 28 2019 Phase 1|Phase 2
NCT02601378 Terminated
Uveal Melanoma
Novartis Pharmaceuticals|Novartis
 February 1 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 472.47 Formula

C22H23F3N8O
CAS No. 1874276-76-2 SDF --
Smiles CC1(CCN(CC1)C2=C(N=CC=C2)NC(=O)C3=NC(=CN=C3N)C4=C(C=CC=N4)C(F)(F)F)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 94 mg/mL ( (198.95 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 47 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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