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LXH254 [1800398-38-2]

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Référence NB-64-03234-1mL

Conditionnement : 1mLx10mM(inDMSO)

Marque : Neo Biotech

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LXH254

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Synonyms:

Catalog No. T11898 Copy Product Info

Purity: 99.92%

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

Cas No. 1800398-38-2

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.92%

Color:White to Yellow

Product Information

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	ARAF:6.4 nM (IC50), B-Raf:0.21 nM (IC50), Abl-1:4.9 μM (IC50), p38α:2.1 μM (IC50), Raf:0.072 nM (IC50)
In vitro	Method: 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™. Result LXH254 inhibited 80% of the kinases in HCT 116 cells ^[1]. Method: 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. Result LXH254 effectively inhibited RAF signaling in the insensitive model tested ^[1].
In vivo	Method: 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. Result 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

Powder: -20°C for 3 years | 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: 10 mg/mL (19.9 mM), Suspension.

10% DMSO+90% Saline: < 10 mg/mL (19.9 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

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

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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

Keywords

SelectiveRaf kinasesRafp38 MAPKMia PaCa-2MEL-JUSOLXH-254LXH254LXH 254InhibitorinhibitHCT116C-RafB-RafBcr-AblA375

Related Tags: LXH254 chemical structure | LXH254 in vivo | LXH254 in vitro | LXH254 formula | LXH254 molecular weight