LY-2584702 free base
Based on 6 publication(s) in Google Scholar
LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
For research use only. We do not sell to patients.
- CAS No.: 1082949-67-4
- Formula: C21H19F4N7
- Molecular Weight:445.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LY-2584702 free base
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Customer Validation & Images
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Histological Imaging/Staining
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In Vivo Efficacy Study
Biological Activity
Description
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p70S6K 4 nM (IC50) |
In Vitro
LY-2584702 (LY2584702) inhibits phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC50 of 0.1-0.24 μM[1]. For pS6 inhibition in cells, the IC50=100 nM. LY-2584702 has some activity against the S6K-related kinases MSK2 and RSK at high concentrations (enzyme assay IC50=58-176 nM). LY-2584702 inhibits S6K activity in EOMA cells, as determined by the phosphorylation of its downstream effector S6, in a dose-dependent manner[2]. Proliferation of A549 is significantly inhibited by LY-2584702 (LY2584702) treating over 24 h at 0.1 μM (P<0.05); and the trend of decline is more conspicuous with longer treatment and/or with the increased drug concentration (all P<0.05). Similar results are also observed in SK-MES-1, although the obvious inhibition is led by LY-2584702 at 0.6 μM (P<0.05), much higher than that of A549[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1082949-67-4
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Appearance Solid
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Molecular Weight 445.42
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Formula C21H19F4N7
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Color Light yellow to yellow
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SMILES
CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Immunity
The chemokine CCL1 triggers an AMFR-SPRY1 pathway that promotes differentiation of lung fibroblasts into myofibroblasts and drives pulmonary fibrosis. [Abstract]2021 Sep 14;54(9):2042-2056.e8. PMID: 34407391
LY-2584702 free base purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Sep 14;54(9):2042-2056.e8. [Abstract]
Masson staining of CCL1-challenged mice along with ERK inhibitor or p70S6K inhibitor LY-2584702 tosylate salt (10 mg/kg; i.p. twice daily for 14 days after the last CCL1 challenge) treatment (n = 5–8, representative of two assays). The results showed that LY-2584702 tosylate salt reduced collagen deposition. Scale bars, 1 mm.
LY-2584702 free base purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Sep 14;54(9):2042-2056.e8. [Abstract]
Crs of CCL1-challenged mice along with ERK inhibitor SCH772984 or p70S6K inhibitor LY-2584702 tosylate salt (10 mg/kg; i.p. twice daily for 14 days after the last CCL1 challenge) treatment (n = 5–8, representative of two assays). The results showed that LY-2584702 tosylate salt improved lung function.
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Hepatology
2023 May 1;77(5):1580-1592. PMID: 36129070 -
Theranostics
Overcoming resistance to EGFR monotherapy in HNSCC by identification and inhibition of individualized cancer processes. [Abstract]2022 Jan 1;12(3):1204-1219. PMID: 35154483
LY-2584702 free base purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Jan 1;12(3):1204-1219. [Abstract]
(upper panel) Cells were treated every three days and regrowth was measured up to 21 days with either monotherapy (erlotinib 0.1 μM (Er), LY-2584702 tosylate salt (LY) 35 μM, TOFA (T) 5 μM), the predicted drug combination (marked with an asterisk) or with the combinations that were predicted to partially target the unbalanced signaling flux of SCC25. Representative methylene blue-stained cell cultures are shown. (lower panel) Regrowth was quantified and presented as a heatmap. Day 0 represents the amount of cells seeded at the same day and was defined as 100%. Fold change relative to the amount of cells at day 0 is presented. Green color indicates higher regrowth levels (> 100%) and red shows decrease or depletion of the cells (< 100%).
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Pharmacol Res
Dihydroartemisinin ameliorates retinal vascular dysfunction in diabetes mellitus via the FASN/Kmal-mTOR/SREBP1 feedback loop. [Abstract]2021 Oct 4;105871. PMID: 34619345 -
Dev Cell
2025 Nov 27:S1534-5807(25)00691-4. PMID: 41314217
LY-2584702 free base purchased from MedChemExpress. Usage Cited in: Dev Cell. 2025 Nov 27:S1534-5807(25)00691-4. [Abstract]
Fluorescence-activated cell sorting (FACS) analysis of naive CD8+ T cells activated in the presence of PLP, either without (DMSO) or with 50 nM LY-2584702 tosylate salt as indicated (n = 6 independent experiments).
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Mol Cell Biochem
MELK inhibits cuproptosis in diffuse large B-cell lymphoma cells via the PI3K/mTOR/S6K-DLAT signaling axis. [Abstract]2026 Jun 2. PMID: 42228272
Solvent & Solubility
In Vitro:
DMSO : ≥ 4.5 mg/mL (10.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 1 mg/mL (2.25 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75. [Content Brief]
[2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50. [Content Brief]
[3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO | 1 mM | 2.2451 mL | 11.2254 mL | 22.4507 mL | 56.1268 mL |
| DMSO | 5 mM | 0.4490 mL | 2.2451 mL | 4.4901 mL | 11.2254 mL |
| 10 mM | 0.2245 mL | 1.1225 mL | 2.2451 mL | 5.6127 mL |
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