Encorafenib (Synonyms: LGX818)

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

製品番号: HY-15605 純度: 99.83%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1269440-17-6

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 124	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 124	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$58	在庫あり	Estimated Time of Arrival: December 31
5 mg	$104	在庫あり	Estimated Time of Arrival: December 31
10 mg	$150	在庫あり	Estimated Time of Arrival: December 31
25 mg	$250	在庫あり	Estimated Time of Arrival: December 31
50 mg	$450	在庫あり	Estimated Time of Arrival: December 31
100 mg	$750	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 45 publication(s) in Google Scholar

Other Forms of Encorafenib:

Encorafenib-¹³C,d₃ 在庫あり
Encorafenib (Standard) お問い合わせ

顧客検証

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.

Raf アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

B-Raf C-Raf Raf

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

体外実験

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.

臨床実験

分子量

540.01

分子式

C₂₂H₂₇ClFN₇O₄S

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

純度とドキュメンテーション

純度: 99.93%

Select Batch:

データシート (277 KB) SDS (393 KB)

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

取扱説明書 (2659 KB)

参考文献

[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]

細胞実験	MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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

最近チェックした製品:

製品名

カスタマ需要量 *

お名前 *

タイトル

メールアドレス *

電話番号 *

デパートメント

組纖名 *

市区町村

都道府県

国或いは地域 *

必ず会社名を記載ください。個人への返信は行いません。

備考

製品名

Lot #

お名前 *

メールアドレス *

電話番号 *

部門 *

組纖名 *

国或いは地域 *

備考

Encorafenib (Synonyms: LGX818)

カスタマーレビュー

Other Forms of Encorafenib:

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Raf アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Encorafenib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

お名前
メール *

	Sorry, but the email address you supplied was invalid.

Encorafenib (Synonyms: LGX818)

カスタマーレビュー

Other Forms of Encorafenib:

Encorafenib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Raf アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Encorafenib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Encorafenib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report