Encorafenib (Synonyms: LGX818)

Name: Encorafenib
Brand: MedChemExpress
SKU: HY-15605
Rating: 5.0 (45 reviews)

Cat. No.: HY-15605 Purity: 99.83%: Data Sheet
COA

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

For research use only. We do not sell to patients.

CAS No. : 1269440-17-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 45 publication(s) in Google Scholar

Other Forms of Encorafenib:

Encorafenib-¹³C,d₃ In-stock
Encorafenib (Standard) Get quote

45 Publications Citing Use of MCE Encorafenib

Cell Proliferation/Viability Assay

Cell Imaging/Staining

Microbiological Assay

In Vivo Efficacy Study

Histological Imaging/Staining

: 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.

: 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.

: 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.

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B-Raf C-Raf Raf

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

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.

Clinical Trial

Molecular Weight

540.01

Formula

C₂₂H₂₇ClFN₇O₄S

CAS No.

1269440-17-6

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (254 KB) HNMR (203 KB) RP-HPLC (232 KB)

Handling Instructions (2659 KB)

References

[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]

Cell Assay	MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Encorafenib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Encorafenib1269440-17-6LGX818LGX 818LGX-818RafRaf kinasesInhibitorinhibitorinhibit

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Encorafenib (Synonyms: LGX818)

Customer Review

Other Forms of Encorafenib:

Encorafenib Related Antibodies

45 Publications Citing Use of MCE Encorafenib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Raf Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Encorafenib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Encorafenib Related Classifications

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