LXH254 [1800398-38-2]

Referencia NB-64-03234-1mL

embalaje : 1mLx10mM(inDMSO)

Marca : Neo Biotech

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Teléfono : +1 850 650 7790

LXH254

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.

LXH254

Copy Product Info

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

LXH254
Cas No. 1800398-38-2
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Purity:99.92%
Color:White to Yellow
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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
p38α:2.1 μM (IC50), ARAF:6.4 nM (IC50), Abl-1:4.9 μM (IC50), Raf:0.072 nM (IC50), B-Raf:0.21 nM (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 Weight502.49
FormulaC25H25F3N4O4
Cas No.1800398-38-2
SmilesCc1ccc(NC(=O)c2ccnc(c2)C(F)(F)F)cc1-c1cc(OCCO)nc(c1)N1CCOCC1
Relative Density.1.353 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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: 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
1mg5mg10mg50mg
1 mM1.9901 mL9.9504 mL19.9009 mL99.5045 mL
5 mM0.3980 mL1.9901 mL3.9802 mL19.9009 mL
10 mM0.1990 mL0.9950 mL1.9901 mL9.9504 mL
20 mM0.0995 mL0.4975 mL0.9950 mL4.9752 mL
50 mM0.0398 mL0.1990 mL0.3980 mL1.9901 mL
100 mM0.0199 mL0.0995 mL0.1990 mL0.9950 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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