| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
LXR623 (WAY-252623; LXR-623) is a novel, highly brain-penetrant, selective and orally bioavailable synthetic modulator of LXR (Liver X receptor) with anticancer activity, It is a partial LXRα and full LXRβ agonist with IC50s of 24 nM and 179 nM, respectively. As a LXRα-partial/LXRβ-full agonist, LXR623 selectively kills GBM cells in an LXRβ- and cholesterol-dependent fashion, causing tumor regression and prolonged survival in mouse models. LXR623 displayed high efficacy in reducing lesion progression in the murine LDLR(-/-) atherosclerosis model with no associated increase in hepatic lipogenesis either in this model or Syrian hamsters. LXR-623 potently kills U87EGFRvIII and GBM39 cells in vitro while completely sparing NHAs. LXR-623 also increases ABCA1 protein and decreases LDLR protein levels in all three cell lines.
| ln Vitro |
In vitro, LXR-623 completely protects NHA while killing U87EGFRvIII and GBM39 cells efficiently. In all three cell lines, LXR-623 also caused an increase in ABCA1 protein and a decrease in LDLR protein levels. In every GBM sample examined, LXR-623 caused massive cell death, upregulated the expression of the ABCA1 efflux transporter, and inhibited the expression of LDLR. By activating LXRβ, LXR-623 (5 μM) also causes GBM cell death[1]. When human PBMCs were treated with LXR-623 in vitro, the transcription of ABCA1 and ABCG1 was markedly elevated [4].
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| ln Vivo |
With little peripheral activity, LXR-623 (400 mg/kg, po) penetrates the blood-brain barrier, triggers the expression of the target gene, and reaches processing levels in GBM cells in the brain. LXR-623 prolongs the survival of mice with intracranial patient-derived GBMs by suppressing tumor growth and promoting tumor cell death [1]. When compared to a placebo, LXR-623 (1.5, 5 mg/kg/day) dramatically slowed the advancement of atherosclerosis in animals [2]. A dose-dependent manner was observed in the significant reduction of atherosclerosis by WAY-252623 (15 and 50 mg/kg). In Syrian hamsters that express CETP, WAY-252623 (20, 60, and 120 mg/kg/day, po) exhibits neutral lipid effects [3]. Additionally, rats' peripheral blood cells showed increased gene expression in response to LXR-623 (50 mg/kg). In monkey whole blood cells, LXR-623 (0, 15 and 50 mg/kg) dose-dependently and proportionately increases the transcription of ABCA1 and ABCG1 [4].
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| References |
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| Molecular Formula |
C21H12CLF5N2
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| Molecular Weight |
422.78
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| Exact Mass |
422.06
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| CAS # |
875787-07-8
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| Related CAS # |
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| PubChem CID |
16734800
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
528.4±50.0 °C at 760 mmHg
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| Melting Point |
100 °C
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| Flash Point |
273.4±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.583
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| LogP |
6.05
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KYWWJENKIMRJBI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H12ClF5N2/c22-18-10-15(24)9-6-13(18)11-29-20(12-4-7-14(23)8-5-12)16-2-1-3-17(19(16)28-29)21(25,26)27/h1-10H,11H2
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| Chemical Name |
2-[(2-chloro-4-fluorophenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)indazole
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3653 mL | 11.8265 mL | 23.6530 mL | |
| 5 mM | 0.4731 mL | 2.3653 mL | 4.7306 mL | |
| 10 mM | 0.2365 mL | 1.1826 mL | 2.3653 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
LXR-623 crosses the blood brain barrier, induces target gene expression, and achieves therapeutic levels in GBM cells in the brain with minimal activity in the periphery.Cancer Cell.2016 Nov 14;30(5):683-693. |
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 LXR-623 kills GBM cells through activation of LXRβ, the dominant subtype in brain tumors.Cancer Cell.2016 Nov 14;30(5):683-693. |
 LXR-623 inhibits tumor growth, promotes tumor cell death and prolongs the survival of mice bearing intracranial patient-derived GBMs.Cancer Cell.2016 Nov 14;30(5):683-693. |
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