Art. -Nr.: HY-12493B

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LY-2584702 hydrochloride

Name: LY-2584702 hydrochloride
Brand: MedChemExpress
SKU: HY-12493B
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6 Cited Publications

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Based on 6 publication(s) in Google Scholar

LY-2584702 hydrochloride 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.

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CAS. Nr.: 1082948-81-9
Formel: C₂₁H₂₀ClF₄N₇
Molecular Weight:481.88

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

LY-2584702 hydrochloride Chemical Structure

CAS. Nr.: 1082948-81-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Protokoll (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LY-2584702 hydrochloride 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.

IC₅₀ & Target

^[1]^[2]

p70S6K

4 nM (IC₅₀)

Alle Ribosomal S6 Kinase (RSK) Isoform-spezifische Produkte anzeigen :

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]. In S6K1 enzyme assay, the IC₅₀ of LY-2584702 (LY2584702) is 2 nM. 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

LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model^[1]. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1082948-81-9
Molecular Weight 481.88
Formel C₂₁H₂₀ClF₄N₇
SMILES

CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (6)

All Histological Imaging/StainingCell Proliferation/Viability AssayFlow CytometryIn Vivo Efficacy Study

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Journal Impact Factor

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 hydrochloride 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 hydrochloride 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.
Hepatology

Interleukin-33 facilitates liver regeneration through serotonin-involved gut-liver axis. [Abstract]

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 hydrochloride 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%).
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

Vitamin B6 preserves the stemness-like phenotypes and antitumor ability of CD8+ T cells. [Abstract]

2025 Nov 27:S1534-5807(25)00691-4. PMID: 41314217

LY-2584702 hydrochloride 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).
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

Protokoll

All Cell Biology

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

LY-2584702 hydrochloride

6 Cited Publications

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LY-2584702 hydrochloride

Publications Citing Use of MedChemExpress (MCE) LY-2584702 hydrochloride

Alle Ribosomal S6 Kinase (RSK) Isoform-spezifische Produkte anzeigen