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LXH254

Name: LXH254
Brand: TargetMol
SKU: T11898
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11898Cas No. 1800398-38-2

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

LXH254

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Purity: 99.92%

Catalog No. T11898Cas No. 1800398-38-2

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$124	In Stock	In Stock
10 mg	$195	In Stock	In Stock
25 mg	$382	In Stock	In Stock
50 mg	$597	In Stock	In Stock
100 mg	$726	In Stock	In Stock
200 mg	$997	-	In Stock
500 mg	$1,520	-	In Stock
1 mL x 10 mM (in DMSO)	$137	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.92%

Color:White to Yellow

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.
Targets&IC50	B-Raf:0.21 nM (IC50), Raf:0.072 nM (IC50), Abl-1:4.9 μM (IC50), ARAF:6.4 nM (IC50), p38α:2.1 μM (IC50)
In vitro	METHODS: HCT 116 cells were treated with LXH254 at 10 µM for 2 hours, and lysates were then processed, probe labeled, and analyzed by LC-MS/MS for intracellular kinase selectivity analysis using KiNativ™. RESULTS LXH254 inhibited 80% of the kinases in HCT 116 cells [1]. METHODS: The sensitivity of WT cell lines to LXH254 was analyzed in a high-throughput format. Use IC50 values in the range 1-2.5 μM. RESULTS LXH254 effectively inhibited RAF signaling in the insensitive model tested [1].
In vivo	METHODS: The anti-tumor effects of LXH254 were tested in a set of BRAF, NRAS and KRAS mutant xenograft models as well as RAS/RAF wild-type models, treated with LXH254 100mgkg orally once daily for one month. RESULTS LXH254 can inhibit the growth of tumor in model mice. [1]

Chemical Properties

Molecular Weight	502.49
Formula	C₂₅H₂₅F₃N₄O₄
Cas No.	1800398-38-2
Smiles	Cc1ccc(NC(=O)c2ccnc(c2)C(F)(F)F)cc1-c1cc(OCCO)nc(c1)N1CCOCC1
Relative Density.	1.353 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (248.76 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.98 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9901 mL	9.9504 mL	19.9009 mL	99.5045 mL
5 mM	0.3980 mL	1.9901 mL	3.9802 mL	19.9009 mL
10 mM	0.1990 mL	0.9950 mL	1.9901 mL	9.9504 mL
20 mM	0.0995 mL	0.4975 mL	0.9950 mL	4.9752 mL
50 mM	0.0398 mL	0.1990 mL	0.3980 mL	1.9901 mL
100 mM	0.0199 mL	0.0995 mL	0.1990 mL	0.9950 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc