Cat. No.: HY-15605

Encorafenib

(Synonyms: LGX818)

47 Cited Publications

Avis client

Based on 47 publication(s) in Google Scholar

Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF^V600E (EC₅₀=4 nM).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.94%
CAS No.: 1269440-17-6
Formule: C₂₂H₂₇ClFN₇O₄S
Masse moléculaire:540.01

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Encorafenib Chemical Structure

CAS No.: 1269440-17-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Essai clinique
Chemical Information
Publications (47)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF^V600E (EC₅₀=4 nM).

IC₅₀ & Target

IC50: 0.3 nM (BRaf^V600E)

Voir tous les produits spécifiques à Isoform Raf :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	EC₅₀	4 nM Compound: Braftovi	Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as reduction in cell growth Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as reduction in cell growth	[PMID: 37944387]

In Vitro

Encorafenib (LGX818) is a potent drug that can prevents diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf^[1]. Encorafenib (LGX818) (10 nM) suppresses the ERK/MAPK pathway and displays marked inhibition of pERK in A375, G361 and SK-MEL-24 cells. 10 nM Encorafenib (LGX818) treatment for 12 days potently inhibits colony formation in A375, G361 and SK-MEL-24 cells, but not in RPMI7951 and C8161 cells. Encorafenib (LGX818) treatment induces a steady increase in the β-catenin level in G361 cells over time^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1269440-17-6
Appearance Solid
Masse moléculaire 540.01
Formule C₂₂H₂₇ClFN₇O₄S
Color Off-white to yellow
SMILES

O=C(OC)N[C@@H](C)CNC1=NC=CC(C2=CN(C(C)C)N=C2C3=CC(Cl)=CC(NS(=O)(C)=O)=C3F)=N1
Synonyms

LGX818
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (47)

All Cell Proliferation/Viability AssayCell Imaging/StainingMicrobiological AssayIn Vivo Efficacy StudyHistological Imaging/StainingWB

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Journal Impact Factor

Signal Transduct Target Ther

BRAF inhibitors enhance erythropoiesis and treat anemia through paradoxical activation of MAPK signaling. [Abstract]

2024 Dec 2;9(1):338. PMID: 39617757

Encorafenib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]

BRAF inhibitors promoted the self-renewal of primary erythroid progenitors in vitro. The drug dose-response assay for UCB-CD34⁺-derived erythroid culture was conducted, with total cell numbers counted on Day 12. The graph illustrates the fold difference in proliferation between the GDC-treated and control (DMSO) groups on Day 12. The dashed line indicates the fold change for the control group. All experiments used control (DMSO), SB-590885 (HY-10966) at 1 μM, GDC-0879 (HY-50864) at 2 μM, and Encorafenib (HY-15605) at 0.5 μM.

Encorafenib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]

Statistical analysis of the area of 75 individual erythroid colonies in panel on Day 14.All experiments used control (DMSO), SB-590885 (HY-10966) at 1 μM, GDC-0879 (HY-50864) at 2 μM, and Encorafenib (HY-15605) at 0.5 μM.

Encorafenib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]

Immunoblotting of MAPK signaling cascade proteins in UCB-CD34⁺-derived erythroblasts cultured under normal conditions and treated on Day 9 with Encorafenib (HY-15605; 0.5 μM), GDC-0879 (HY-50864; 2 μM), or SB-590885 (HY-10966; 0.5 μM) for 30 min.

Encorafenib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]

Levels of phosphorylated and total ERK proteins in UCB-CD34⁺-derived erythroblasts on Day 9, cultured under normal conditions and treated with different BRAF inhibitors (SB-590885 (HY-10966), GDC-0879 (HY-50864), Encorafenib (HY-15605)) for 30 min.
Mol Cancer

LSD1 inhibition attenuates targeted therapy-induced lineage plasticity in BRAF mutant colorectal cancer. [Abstract]

2025 Apr 23;24(1):122. PMID: 40264166
Cancer Discov

A plastic EMP1⁺ to LGR5⁺ cell state conversion as a bypass to KRAS-G12D pharmacological inhibition in metastatic colorectal cancer. [Abstract]

2025 Oct 21. PMID: 41128661
Cancer Res

CFT1946 is an Orally Available Brain-Penetrant BRAFV600-Mutant Degrader that Overcomes BRAF Inhibitor Resistance. [Abstract]

2025 Oct 28. PMID: 41150906
Cancer Res

Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis. [Abstract]

2022 Jul 18;82(14):2552-2564. PMID: 35584009
Redox Biol

Inhibition of 6-formylindolo[3,2-b]carbazole metabolism sensitizes keratinocytes to UVA-induced apoptosis: Implications for vemurafenib-induced phototoxicity. [Abstract]

2021 Oct:46:102110. PMID: 34418602
Nat Chem Biol

MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition. [Abstract]

2026 May 12:10.1038/s41589-026-02212-2. PMID: 42120500
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Clin Invest

MOGAT3-Mediated DAG Accumulation Drives Acquired Resistance to Anti-BRAF/EGFR Therapy in BRAFV600E-Mutant Metastatic Colorectal Cancer. [Abstract]

2024 Oct 22;134(24):e182217. PMID: 39436710

Encorafenib purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22;134(24):e182217. [Abstract]

Encorafenib was administered orally (20 mg/kg/day). Mean tumor volumes of BRAFV600E-mutant mCRC PDXs treated with encorafenib and cetuximab relative to baseline (T0) were measured (n = 6).

Encorafenib purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22;134(24):e182217. [Abstract]

Encorafenib was administered orally (20 mg/kg/day). Representative images of H&E, Ki67, Oil Red O, and TUNEL staining were shown.

Encorafenib purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 22;134(24):e182217. [Abstract]

Western blots showing protein expression of MOGAT3 in RKO, RKO EC-R, HT29, and HT29 EC-R cells. Representative blots were shown. MOGAT3KO RKO EC-R and HT29 EC-R, along with RKO EC-R-CTRL and HT29 EC-R-CTRL cell lines, were exposed to 2 μM Encorafenib/4 μM cetuximab for 96 hours.
Adv Sci (Weinh)

Microfluidic Organoid Cultures Derived from Pancreatic Cancer Biopsies for Personalized Testing of Chemotherapy and Immunotherapy. [Abstract]

2024 Feb;11(5):e2303088. PMID: 38018486

Encorafenib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Feb;11(5):e2303088. [Abstract]

Encorafenib (5–10 μM; 7 days). Relative drug response graph for four drug treatment groups after 7 days of treatment (viability %) was presented.

Encorafenib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Feb;11(5):e2303088. [Abstract]

Encorafenib (2.5 μM; 7 days). In situ monitoring of apoptosis in organoids using Caspase 3/7 green assay. Upper images are green fluorescence signals at 48 h and 72 h.
Sci Adv

BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS. [Abstract]

2019 Aug 14;5(8):eaav8463. PMID: 31453322
Clin Cancer Res

Precision Oncology and Systemic Targeted Therapy in Pseudomyxoma Peritonei. [Abstract]

2024 Sep 13;30(18):4082-4099. PMID: 39018564
Proc Natl Acad Sci U S A

Mutation-oriented profiling of autoinhibitory kinase conformations predicts RAF inhibitor efficacies. [Abstract]

2020 Dec 8;117(49):31105-31113. PMID: 33229534
Br J Cancer

Co-targeting SRC overcomes resistance to BRAF inhibitors in colorectal cancer. [Abstract]

2025 Jun 6. PMID: 40481178
Cell Syst

Resistor: An algorithm for predicting resistance mutations via Pareto optimization over multistate protein design and mutational signatures. [Abstract]

2022 Oct 19;13(10):830-843.e3. PMID: 36265469
Mol Cancer Ther

Concurrent inhibition of ICMT and RAF/MEK suppresses RAC1P29S-driven MAPK-pathway-inhibitor resistance in BRAFV600E melanoma by regulating TAZ activity. [Abstract]

2026 Jun 24. PMID: 42338299
Mol Cancer Ther

Mosperafenib, a novel paradox breaker BRAF inhibitor with potent preclinical activity in BRAF mutated colorectal cancer. [Abstract]

2025 Dec 4. PMID: 41340484
Pharmaceutics

Evaluation of Alectinib Metabolic Stability in HLMs Using Fast LC-MS/MS Method: In Silico ADME Profile, P450 Metabolic Lability, and Toxic Alerts Screening. [Abstract]

2023 Oct 11;15(10):2449. PMID: 37896209
Pharmaceutics

Encorafenib Acts as a Dual-Activity Chemosensitizer through Its Inhibitory Effect on ABCC1 Transporter In Vitro and Ex Vivo. [Abstract]

2022 Nov 24;14(12):2595. PMID: 36559089
Cancer Immunol Immunother

Antitumor effects of immunotherapy combined with BRAF and MEK inhibitors in BRAF V600E metastatic colorectal cancer. [Abstract]

2025 Mar 19;74(5):154. PMID: 40105971
Mol Cancer Res

Ruthenium drug BOLD-100 regulates BRAFMT colorectal cancer cell apoptosis through AhR/ROS/ATR signaling axis modulation. [Abstract]

2024 Dec 3;22(12):1088-1101. PMID: 39083088
ACS Appl Bio Mater

Decellularized Dermis ECM-Based Melanoma-on-a-Chip Model with Integrated Lymphatic and Vascular Networks for High-Throughput Drug Testing. [Abstract]

2026 Feb 18. PMID: 41708064
ACS Omega

Synthesis of a 11C-Isotopologue of the B-Raf-Selective Inhibitor Encorafenib Using In-Loop [11C]CO2 Fixation. [Abstract]

2020 Aug 16;5(33):20960-20966. PMID: 32875231
Eur J Pharm Sci

Biophysical and docking study on the interaction of anticancer drugs encorafenib and binimetinib with human serum albumin. [Abstract]

2023 Oct 1:189:106550. PMID: 37527692
Molecules

A Rapid and Sensitive Liquid Chromatography-Tandem Mass Spectrometry Bioanalytical Method for the Quantification of Encorafenib and Binimetinib as a First-Line Treatment for Advanced (Unresectable or Metastatic) Melanoma-Application to a Pharmacokinetic Study. [Abstract]

2022 Dec 22;28(1):79. PMID: 36615272
Molecules

A Validated LC-MS/MS Assay for the Simultaneous Quantification of the FDA-Approved Anticancer Mixture (Encorafenib and Binimetinib): Metabolic Stability Estimation. [Abstract]

2021 May 5;26(9):2717. PMID: 34063139
JCO Precis Oncol

Modeling Extraordinary Response Through Targeting Secondary Alterations in Fusion-Associated Sarcoma. [Abstract]

2024 Jun:8:e2300688. PMID: 38885476
Cancer Res Commun

A Drug Discovery Pipeline for MAPK/ERK Pathway Inhibitors in Caenorhabditis elegans. [Abstract]

2024 Sep 1;4(9):2454-2462. PMID: 39212544
Analyst

Development and validation of a quick and sensitive UPLC-MS/MS method for measuring ensartinib in HLMs: investigation of structural alerts associated with metabolic lability and in silico toxicity. [Abstract]

2025 Nov 17;150(23):5174-5189. PMID: 41195964
Separations

2023 Apr 25, 10(5), 278.
J Pharm Biomed Anal

Estimation of zorifertinib metabolic stability in human liver microsomes using LC-MS/MS. [Abstract]

2022 Mar 20:211:114626. PMID: 35123331
Anal Methods

Developing and validating a sensitive and fast UPLC-MS/MS method for estimating the in vitro metabolic stability of crenolanib in HLMs: identification of structural alarms related to the in silico toxicity and metabolic lability. [Abstract]

2025 Nov 27;17(46):9442-9453. PMID: 41246990
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
J Chem Eng Data

2024 Jun 10.
Onco Targets Ther

Ouabain Exhibited Strong Anticancer Effects in Melanoma Cells via Induction of Apoptosis, G2/M Phase Arrest, and Migration Inhibition. [Abstract]

2021 Feb 25:14:1261-1273. PMID: 33658794
Acta Chromatogr

2025 Feb 25.
Indiana University

2026.
University of Arizona

2025.
bioRxiv

Reprogramming of Cellular Plasticity via ETS and MYC Core-regulatory Circuits During Response to MAPK Inhibition in BRAF-mutant Colorectal Cancer. [Abstract]

2025 Jun 20:2025.06.15.659716. PMID: 40611889
Indiana University

2025.
bioRxiv

A structure-based modelling approach identifies effective drug combinations for RAS-mutant acute myeloid leukemia. [Abstract]

2025 May 3:2025.04.29.651188. PMID: 40654850
Patent

US20240366605A1
bioRxiv

2024 October 29.
Patent

US20240307392A1.
Patent

US20240366605A1.
bioRxiv

2024 September 19.
Research Square Print

December 21st, 2022.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (92.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8518 mL

9.2591 mL

18.5182 mL

5 mM

0.3704 mL

1.8518 mL

3.7036 mL

10 mM

0.1852 mL

0.9259 mL

1.8518 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (4.63 mM); Suspended solution; Need ultrasonic

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 16.67 mg/mL (30.87 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
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Elemental Analysis Report (2659 KB)
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OR (2659 KB)
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Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Compounds and compositions as protein kinase inhibitors . Patent WO 2011025927 A1

[2]. Li Z, et al. Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells. Cancer Lett. 2016 Jan 28;370(2):332-44. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8518 mL	9.2591 mL	18.5182 mL	46.2954 mL
	5 mM	0.3704 mL	1.8518 mL	3.7036 mL	9.2591 mL
	10 mM	0.1852 mL	0.9259 mL	1.8518 mL	4.6295 mL
	15 mM	0.1235 mL	0.6173 mL	1.2345 mL	3.0864 mL
	20 mM	0.0926 mL	0.4630 mL	0.9259 mL	2.3148 mL
	25 mM	0.0741 mL	0.3704 mL	0.7407 mL	1.8518 mL
	30 mM	0.0617 mL	0.3086 mL	0.6173 mL	1.5432 mL
	40 mM	0.0463 mL	0.2315 mL	0.4630 mL	1.1574 mL
	50 mM	0.0370 mL	0.1852 mL	0.3704 mL	0.9259 mL
	60 mM	0.0309 mL	0.1543 mL	0.3086 mL	0.7716 mL
	80 mM	0.0231 mL	0.1157 mL	0.2315 mL	0.5787 mL

Keywords

Encorafenib

47 Cited Publications

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Encorafenib

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Publications Citing Use of MedChemExpress (MCE) Encorafenib

Voir tous les produits spécifiques à Isoform Raf

Activité biologique

Chemical Information

Publications (47)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Encorafenib Related Classifications

HY-15605 Related Classifications