Art. -Nr.: HY-111940

LUT014

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LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy.

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Reinheit: 97.09%
CAS. Nr.: 2274819-46-2
Formel: C₂₇H₁₉F₃N₈O
Molecular Weight:528.49

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

LUT014 Chemical Structure

CAS. Nr.: 2274819-46-2

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Preis

Verfügbarkeit

Menge

Amount: USD 0.00

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

B-Raf

11.7 nM (IC₅₀)

Alle Raf Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

In Vitro

LUT014 (0.3 μM; 2 h) induces elevated levels of phosphorylated ERK1/2 (pERK) in primary human epidermal keratinocytes (HEKa), reverses pERK inhibition induced by Erlotinib (HY-50896) or Cetuximab (HY-P9905), and restores MAPK signaling to levels close to those stimulated by growth factors^[4].
LUT014 (0.002-1.11 μM; 72 h) induces a bell-shaped proliferation curve in KRAS G12C mutant MIA-PaCa-2 pancreatic cancer cells in a concentration-dependent manner, with the strongest proliferation at 0.041 μM, and high concentrations (≥0.37 μmol/L) inhibited proliferation^[4].

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

Western Blot Analysis^[4]

Cell Line:

Primary human epidermal keratinocytes (HEKa cells)
Concentration:

0.3 μM
Incubation Time:

2 h
Result:

Increased the pERK/total ERK2 ratio by 1.8-fold compared to vehicle control (DMSO), reversing the 50% reduction in pERK induced by Erlotinib (10 μM) or Cetuximab (50 μg/mL).
The combination of LUT014 with EGFR inhibitors restored pERK levels to 85% of those stimulated by human keratinocyte growth supplement (HKGS).

Cell Proliferation Assay^[4]

Cell Line:

MIA-PaCa-2 (KRAS G12C-mutated pancreatic cancer cells)
Concentration:

0.002, 0.05, 0.14, 0.41, 1.11 μM
Incubation Time:

72 h
Result:

Significantly enhanced cell proliferation by 40% compared to vehicle control, at 0.041 μM, while concentrations ≥0.37 μmol/L caused growth arrest.
The maximal proliferation at low doses correlated with paradoxical MAPK activation, as demonstrated by increased pERK levels in Western blot analyses.

Clinical Trial

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

Chemical Information

CAS. Nr. 2274819-46-2
Appearance Solid
Molecular Weight 528.49
Formel C₂₇H₁₉F₃N₈O
Color Light yellow to yellow
SMILES

FC(F)(F)OC1=CC(NC2=NC=CC3=C2C=CC(C)=C3NC4=NC=CC=C4C5=C6N=CNC6=NC=N5)=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (94.61 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

1.8922 mL

9.4609 mL

18.9218 mL

5 mM

0.3784 mL

1.8922 mL

3.7844 mL

10 mM

0.1892 mL

0.9461 mL

1.8922 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Katz S, et al. A topical BRAF inhibitor (LUT-014) for treatment of radiodermatitis among women with breast cancer. JAAD Int. 2023 Dec 25;15:62-68. [Content Brief]

[2]. Wang PP, et al. BRAF Mutations in Colorectal Liver Metastases: Prognostic Implications and Potential Therapeutic Strategies. Cancers (Basel). 2022 Aug 23;14(17):4067. [Content Brief]

[3]. Li Y, et al. Mechanism of Lethal Skin Toxicities Induced by Epidermal Growth Factor Receptor Inhibitors and Related Treatment Strategies. Front Oncol. 2022 Feb 10;12:804212. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8922 mL	9.4609 mL	18.9218 mL	47.3046 mL
	5 mM	0.3784 mL	1.8922 mL	3.7844 mL	9.4609 mL
	10 mM	0.1892 mL	0.9461 mL	1.8922 mL	4.7305 mL
	15 mM	0.1261 mL	0.6307 mL	1.2615 mL	3.1536 mL
	20 mM	0.0946 mL	0.4730 mL	0.9461 mL	2.3652 mL
	25 mM	0.0757 mL	0.3784 mL	0.7569 mL	1.8922 mL
	30 mM	0.0631 mL	0.3154 mL	0.6307 mL	1.5768 mL
	40 mM	0.0473 mL	0.2365 mL	0.4730 mL	1.1826 mL
	50 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9461 mL
	60 mM	0.0315 mL	0.1577 mL	0.3154 mL	0.7884 mL
	80 mM	0.0237 mL	0.1183 mL	0.2365 mL	0.5913 mL

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LUT014

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Alle Raf Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LUT014 Related Classifications

HY-111940 Related Classifications