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Purity: ≥98%
LJI308 is a novel, potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with potential antitumor activity. It blocks RSK1, RSK2, and RSK3 with respective IC50 values of 6 nM, 4 nM, and 13 nM. LJI308 overcomes chemoresistance by getting rid of cancer stem cells. It aims to stop the spread of TNBC among the CSC population. LJI308 had little effect on the non-tumorigenic parental HMECs and was specifically directed at transformed cells. The promise of preventing the growth of TNBC is delivered by targeting RSK with specific and powerful inhibitors like LJI308.
| Targets |
RSK2 (IC50 = 4 nM); RSK1 (IC50 = 6 nM); RSK3 (IC50 = 13 nM)
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| ln Vitro |
LJI308 inhibits cell growth in MDA-MB-231 and H358 cells by blocking cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 with an EC50 of 0.2-0.3 M.[1] LJI308 also inhibits YB-1 while suppressing cell growth in TNBC HTRY-LT cells.[2]
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| ln Vivo |
NA
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| Enzyme Assay |
Enzymatic activity of RSK isoforms 1, 2, and 3 is assessed using recombinant full-length RSK protein. RSK1 (1 nM), RSK2 (0.1 nM), or RSK3 (1 nM) is allowed to phosphorylate 200 nM peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1- 5 μM, RSK2- 20 μM, RSK3- 10 μM) and appropriate dilutions of RSK inhibitors in 50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.1% BSA Fraction V, 0.01% Tween-20. An anti-phospho-AKT substrate antibody and AlphaScreen reagents, as directed by the manufacturer, were used to determine the extent of peptide phosphorylation after 150 minutes at room temperature. The reaction was then stopped with 60 mM EDTA.
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| Cell Assay |
Cell growth under attached conditions is assessed by plating 1000 cells per well on 96-well tissue culture-treated plates in cell growth medium. Cell growth was measured after 72 hours by adding CellTiter Glo reagent in accordance with manufacturer's instructions. Appropriate dilutions of the compound are 4 added medium above the cells.
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| Animal Protocol |
NA;
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| References |
| Molecular Formula |
C21H18F2N2O2
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| Molecular Weight |
368.376632213593
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| Exact Mass |
368.1336
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| Elemental Analysis |
C, 68.47; H, 4.93; F, 10.31; N, 7.60; O, 8.69
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| CAS # |
1627709-94-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1COCCN1C2=CC=C(C=C2)C3=C(C=NC=C3)C4=CC(=C(C(=C4)F)O)F
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| InChi Key |
YUYJEQHNWKQNBT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18F2N2O2/c22-19-11-15(12-20(23)21(19)26)18-13-24-6-5-17(18)14-1-3-16(4-2-14)25-7-9-27-10-8-25/h1-6,11-13,26H,7-10H2
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| Chemical Name |
2,6-Difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]-phenol
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| Synonyms |
LJI 308; LJI308; LJI-308; NVP-LJI308; NVP-LJI 308; NVP-LJI-308
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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) |
DMSO: ~73 mg/mL (~198.2 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 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 | 2.7146 mL | 13.5729 mL | 27.1459 mL | |
| 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL | |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 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.
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