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Purity: ≥98%
LY2584702 is a novel, selective, orally bioavailable, and ATP-competitive inhibitor of p70S6K (ribosomal p70 S6 kinase) with potential antitumor activity. It inhibits p70S6K with an IC50 of 4 nM. By inhibiting ribosomal protein S6 kinase (p70S6K) and preventing the phosphorylation of the S6 subunit of ribosomes, LY2584702 demonstrated strong antiproliferative activity in vitro and high antitumor efficacy in vivo. This inhibition of normal ribosomal function within tumor cells results in a reduction in protein synthesis and cellular proliferation.
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 M.[1] LY2584702 inhibits the phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC50 of 0.1-0.24 M.[1]
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ln Vivo |
In the xenograft models of U87MG glioblastoma and HCT116 colon carcinoma, LY2584702 (12.5 mg/kg BID) exhibits significant antitumor efficacy. [1]
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Enzyme Assay |
LY2584702 Tosylate (also known as LYS6K2) is a novel, selective, orally bioavailable, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
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Cell Assay |
Cells were treated with indicated concentration of drug for 24 h.
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Animal Protocol |
U87MG glioblastoma and HCT116 colon carcinoma xenograft models
12.5 mg/kg BID |
References |
Molecular Formula |
C21H19F4N7
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Molecular Weight |
445.4256
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Exact Mass |
445.1638
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Elemental Analysis |
C, 56.63; H, 4.30; F, 17.06; N, 22.01
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CAS # |
1082949-67-4
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Related CAS # |
LY-2584702 tosylate salt;1082949-68-5;LY-2584702 hydrochloride;1082948-81-9
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Appearance |
Solid powder
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SMILES |
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 |
FYXRSVDHGLUMHB-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H19F4N7/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/h2-3,8-12H,4-7H2,1H3,(H,26,27,28,30)
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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
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Synonyms |
LYS6K2; LY 2584702; LY-2584702; LY2584702; LYS 6K2; LYS-6K2
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HS Tariff Code |
2934.99.03.00
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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: ~1 mg/mL (~2.2 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2450 mL | 11.2251 mL | 22.4502 mL | |
5 mM | 0.4490 mL | 2.2450 mL | 4.4900 mL | |
10 mM | 0.2245 mL | 1.1225 mL | 2.2450 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.
NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01241461 | Completed | Drug: LY2584702 | Cancer | Eli Lilly and Company | November 2010 | Phase 1 |
NCT01372085 | Completed | Drug: Placebo Drug: LY2584702 Test Formulation |
Healthy Participants | Eli Lilly and Company | June 2011 | Phase 1 |
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. td> |
Proliferation alteration of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702 (CCK-8 analysis).PLoS One.2017 Aug 9;12(8):e0182891. td> |
Cell cycle distribution of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702.PLoS One.2017 Aug 9;12(8):e0182891. td> |