| 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 |
p70S6K (IC50 = 4 nM)
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|---|---|
| ln Vitro |
LY2584702 inhibits the phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC50 of 0.1-0.24 μM. [1] When combined with the mTOR inhibitor everolimus or the EGFR inhibitor erlotinib, LY2584702 exhibits notable synergistic effects. [2]
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| ln Vivo |
In both the U87MG glioblastoma and the HCT116 colon carcinoma xenograft models, LY2584702 (12.5 mg/kg BID) exhibits significant antitumor efficacy.[1]
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| Cell Assay |
LY-2584702 is completely dissolved in 20 mL of 10% DMSO and stored at -80°C. When conducting the experiments in vitro, LY-2584702 is further diluted in 0.5% Tween 80, 5% propylene glycol, and 30% PEG400 to achieve various DMSO concentrations of 0.1 μM, 0.2 μM, 0.6 μM, and 1.0 μM. In vitro cell proliferation is assessed using the Cell Counting Kit-8 (CCK-8). A549 and SK-MES-1 cell lines that have been exposed to LY-2584702 at various concentrations for 24 hours are seeded in 96-well plates at a density of 5 103 cells per well with six repetitions. The concentration of LY-2584702 at zero is used as a negative control, or DMSO treated. Every 24 hours after seeding, cells' absorbance at 450 nm is measured to gauge their proliferative activities.
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| Animal Protocol |
Mice; LY-2584702 is prepared in 0.25% Tween-80 and 0.05% antifoam, and administered orally to mice (12.5 mg/kg twice daily). Injections of EOMA cells (0.3×106) are made subcutaneously into nu/nu female mice aged 6 to 8 weeks (2 sites/mouse, 4-5 mice/group). Every day, the tumor's size is determined. Animals are either given a vehicle control or the drug LY-2584702 (12.5 mg/kg twice daily, oral dosing) for treatment when tumors grow to a size of 0.01 cm3. Every 3–4 days, tumor size is determined.
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| References |
| Molecular Formula |
C28H27F4N7O3S
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|---|---|
| Molecular Weight |
617.62
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| Exact Mass |
445.1638
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| Elemental Analysis |
C, 54.45; H, 4.41; F, 12.30; N, 15.88; O, 7.77; S, 5.19
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| CAS # |
1082949-68-5
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| Related CAS # |
LY-2584702 free base;1082949-67-4;LY-2584702 hydrochloride;1082948-81-9
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| Appearance |
White to off-white solid powder
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.CN1C=C(N=C1C2CCN(CC2)C3=NC=NC4=C3C=NN4)C5=CC(=C(C=C5)F)C(F)(F)F
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| InChi Key |
HDYUXDNMHBQKAU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19F4N7.C7H8O3S/c1-31-10-17(13-2-3-16(22)15(8-13)21(23,24)25)29-19(31)12-4-6-32(7-5-12)20-14-9-28-30-18(14)26-11-27-20;1-6-2-4-7(5-3-6)11(8,9)10/h2-3,8-12H,4-7H2,1H3,(H,26,27,28,30);2-5H,1H3,(H,8,9,10)
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| Chemical Name |
4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methylimidazol-2-yl]piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine;4-methylbenzenesulfonic acid
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| Synonyms |
LYS6K2 tosylate; LY2584702; LY 2584702; LY-2584702; LYS-6K2; LYS 6K2; LY2584702 tosylate
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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: ~7 mg/mL (~11.3 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6191 mL | 8.0956 mL | 16.1912 mL | |
| 5 mM | 0.3238 mL | 1.6191 mL | 3.2382 mL | |
| 10 mM | 0.1619 mL | 0.8096 mL | 1.6191 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.
Protein expression of RPS6KB1, p-RPS6KB1, rpS6 and p-rpS6 after the treatment by various LY2584702 concentrations for 24 h.PLoS One.2017 Aug 9;12(8):e0182891. |
Proliferation alteration of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702 (CCK-8 analysis).PLoS One.2017 Aug 9;12(8):e0182891. |
Cell cycle distribution of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702.PLoS One.2017 Aug 9;12(8):e0182891. |
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