Size | Price | Stock | Qty |
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1mg |
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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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250mg |
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Other Sizes |
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Purity: ≥98%
Targets |
RSK1 (IC50 = 6 nM); RSK1 (IC50 = 5 nM); RSK1 (IC50 = 4 nM)
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ln Vitro |
LJH685 (0.01-100 μM; 72 hours) has effective EC50 values of 0.73 and 0.79 μM, respectively, for inhibiting the growth of MDA-MB-231 and H358 cells in soft agar.
LJH685 (0.1-10 μM; 4 hours) efficient at submicromolar concentrations and nearly completely inhibits YB1 phosphorylation at higher concentrations[1]. |
Enzyme Assay |
Recombinant full-length RSK protein is used to measure the enzymatic activity of RSK isoforms 1, 2, and 3 (PV4049, PV4051, and PV3846). RSK1 (1 nmol/L), RSK2 (0.1 nmol/L), or RSK3 (1 nmol/L) is allowed to phosphorylate 200 nmol/L peptide substrate (biotin-AGAGRSRHSSYPAGT-OH) in the presence of ATP at concentration equal to the Km for ATP for each enzyme (RSK1, 5 μmol/L; RSK2, 20 μmol/L; and RSK3, 10 μmol/L) and appropriate dilutions of RSK inhibitors.
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Cell Assay |
By seeding 1000 cells per well on 96-well tissue culture-treated plates with cell growth medium, it is possible to measure cell growth under the attached conditions. After 72 hours, cell growth is evaluated by adding CellTiter Glo reagent in accordance with manufacturer's instructions. Appropriate dilutions of the compound are added to the medium above the cells.
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References |
Molecular Formula |
C22H21F2N3O
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Molecular Weight |
381.42
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Exact Mass |
381.1653
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Elemental Analysis |
C, 69.28; H, 5.55; F, 9.96; N, 11.02; O, 4.19
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CAS # |
1627710-50-2
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Related CAS # |
1627710-50-2
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Appearance |
Solid powder
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SMILES |
CN1CCN(CC1)C2=CC=C(C=C2)C3=C(C=NC=C3)C4=CC(=C(C(=C4)F)O)F
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InChi Key |
IKUFKDGKRLMXEX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3
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Chemical Name |
2,6-difluoro-4-[4-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]phenol
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Synonyms |
LJH685; LJH685; LJH685; NVP LJH685; NVP-LJH685;NVPLJH685; NVP LJH 685; NVP-LJH-685
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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 |
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: ~20 mg/mL (~52.4 mM)
Ethanol: ~10mg/mL (~26.2 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.62 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL | |
5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | |
10 mM | 0.2622 mL | 1.3109 mL | 2.6218 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.
LJH685 and LJI308 are potent and specific RSK inhibitors. Mol Cancer Res . 2014 May;12(5):803-12. td> |
Crystal structure of LJH685 bound to RSK2 confirms binding to the ATP site with pyridine nitrogen as the hinge binder. Mol Cancer Res . 2014 May;12(5):803-12. td> |
LJH685 modulates YB1 phosphorylation but affects phosphorylation of S6RP only in combination with mTOR inhibitors. Mol Cancer Res . 2014 May;12(5):803-12. td> |