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Plixorafenib (PLX8394) Raf inhibitor

Name: Plixorafenib (PLX8394)
SKU: S7965
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S7965

Plixorafenib (PLX8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.

Chemical Structure

Molecular Weight: 542.53

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.28%

99.28

Related Targets	Ras ERK p38 MAPK JNK MEK S6 Kinase MAP4K TAK1 Mixed Lineage Kinase ASK MNK MAPKAPK2 KLF TOPK
Related Products	PLX-4720 LY3009120 AZ 628 GDC-0879 SB590885 TAK-632 RAF265 (CHIR-265) GW5074 Avutometinib (Ro 5126766) PLX7904 ZM 336372 Naporafenib (LXH254) Lifirafenib (BGB-283) Agerafenib (CEP-32496) Tovorafenib (MLN2480) Belvarafenib B-Raf inhibitor 1 (Compound 13) dihydrochloride RAF709 CCT196969 RKIP Antibody [E4D22] HG6-64-1 Tinlorafenib TBAP-001 Flezurafenib GNE-9815 Phospho-c-Raf (Ser338) Antibody [F15C8] B-Raf IN 1 Raf inhibitor 1 c-Raf Antibody [E17B21] RG6344

Chemical Information, Storage & Stability

Molecular Weight	542.53	Formula	C₂₅H₂₁F₃N₆O₃S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1393466-87-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC1C2=NC=C(C=N2)C3=CC4=C(NC=C4C(=O)C5=C(C=CC(=C5F)NS(=O)(=O)N6CCC(C6)F)F)N=C3

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (184.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	BRAF(V600E) ^[2] (Cell-free assay) 3.8 nM BRAF ^[2] (Cell-free assay) 14 nM CRAF ^[2] (Cell-free assay) 23 nM
In vitro	PLX8394 is a next-generation, orally available small-molecule BRAFi that does not induce the RAF/MEK/ERK paradoxical activation and blocks signaling from both monomeric BRAF^V600 and dimeric BRAF^{non-V600 protein}^[1].
In vivo	PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with potential antineoplastic activity.
References	[1] http://mct.aacrjournals.org/content/17/1_Supplement/B176 [2] https://pubmed.ncbi.nlm.nih.gov/26466569/ [3] https://pubmed.ncbi.nlm.nih.gov/28659148/ [4] https://pubmed.ncbi.nlm.nih.gov/34108213/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-MEK / p-ERK / ERK		30559419

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02012231	Terminated	Melanoma\|Thyroid Cancer\|Colorectal Cancer\|Non-small Cell Lung Cancer\|Cholangiocarcinoma\|Histiocytosis\|Hairy Cell Leukemia	Fore Biotherapeutics	February 2014	Phase 1

Tech Support

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