MedKoo Cat#: 206867 | Name: LY2584702 free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LY-2584702, also known as LYS6K2, is an orally available inhibitor of p70S6K signaling, with potential antineoplastic activity. LY2584702 inhibits ribosomal protein S6 Kinase (p70S6K), and prevents phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation. P70S6K, a serine/threonine kinase, acts downstream of PIP3 and phosphoinositide-dependent kinase-1 in the PI3 kinase pathway, is often upregulated in a variety of cancer cells, and is involved in the regulation of cell growth, proliferation, motility, and survival.

Chemical Structure

LY2584702 free base
LY2584702 free base
CAS#1082949-67-4 (free base)

Theoretical Analysis

MedKoo Cat#: 206867

Name: LY2584702 free base

CAS#: 1082949-67-4 (free base)

Chemical Formula: C21H19F4N7

Exact Mass: 445.1638

Molecular Weight: 445.43

Elemental Analysis: C, 56.63; H, 4.30; F, 17.06; N, 22.01

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Synonym
LY2584702; LY 2584702; LY-2584702; LYS6K2; LYS-6K2; LYS 6K2; LY2584702
IUPAC/Chemical Name
4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine
InChi Key
FYXRSVDHGLUMHB-UHFFFAOYSA-N
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)
SMILES Code
CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
Product Data
Biological target:
LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM.
In vitro activity:
To illustrate the underlying mechanism of RPS6KB1 phosphorylation in NSCLC, LY2584702 was employed to inhibit the RPS6KB1 phosphorylation specifically both in lung adenocarcinoma cell line A549 and squamous cell carcinoma cell line SK-MES-1. As expected, RPS6KB1 dephosphorylation remarkably suppressed cells proliferation in CCK-8 test, and promoted more cells arresting in G0-G1 phase by cell cycle analysis. Reference: PLoS One. 2017 Aug 9;12(8):e0182891. https://pubmed.ncbi.nlm.nih.gov/28792981/
In vivo activity:
In Long Evans diet-induced obese (DIO) rats, oral administration of LY2584702 for 3-4 weeks led to robust reduction of LDL-C up to 60%. Reference: J Pharmacol Exp Ther. 2017 Jul;362(1):108-118. https://pubmed.ncbi.nlm.nih.gov/28465372/
Solvent mg/mL mM
Solubility
DMSO 4.5 10.10
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 445.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Naito K, Kurihara K, Moteki H, Kimura M, Natsume H, Ogihara M. Effect of Selective Serotonin (5-HT)2B Receptor Agonist BW723C86 on Epidermal Growth Factor/Transforming Growth Factor-α Receptor Tyrosine Kinase and Ribosomal p70 S6 Kinase Activities in Primary Cultures of Adult Rat Hepatocytes. Biol Pharm Bull. 2019 Apr 1;42(4):631-637. doi: 10.1248/bpb.b18-00831. Epub 2019 Feb 1. PMID: 30713268. 2. Chen B, Yang L, Zhang R, Gan Y, Zhang W, Liu D, Chen H, Tang H. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891. doi: 10.1371/journal.pone.0182891. PMID: 28792981; PMCID: PMC5549961. 3. Estridge TB, Dey AB, Reidy C, Yu X, Zhang Y, Hartley M, Milligan PL, Jin N, Kowala MC, Leohr JK, Fretland AJ, Mabry TE, Luffer-Atlas D, Luo MJ. Identification of 4-Aminopyrazolopyrimidine Metabolite That May Contribute to the Hypolipidemic Effects of LY2584702 in Long Evans Diet-Induced Obese Rats. J Pharmacol Exp Ther. 2017 Jul;362(1):108-118. doi: 10.1124/jpet.117.240242. Epub 2017 May 2. PMID: 28465372.
In vitro protocol:
1. Naito K, Kurihara K, Moteki H, Kimura M, Natsume H, Ogihara M. Effect of Selective Serotonin (5-HT)2B Receptor Agonist BW723C86 on Epidermal Growth Factor/Transforming Growth Factor-α Receptor Tyrosine Kinase and Ribosomal p70 S6 Kinase Activities in Primary Cultures of Adult Rat Hepatocytes. Biol Pharm Bull. 2019 Apr 1;42(4):631-637. doi: 10.1248/bpb.b18-00831. Epub 2019 Feb 1. PMID: 30713268. 2. Chen B, Yang L, Zhang R, Gan Y, Zhang W, Liu D, Chen H, Tang H. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891. doi: 10.1371/journal.pone.0182891. PMID: 28792981; PMCID: PMC5549961.
In vivo protocol:
1. Estridge TB, Dey AB, Reidy C, Yu X, Zhang Y, Hartley M, Milligan PL, Jin N, Kowala MC, Leohr JK, Fretland AJ, Mabry TE, Luffer-Atlas D, Luo MJ. Identification of 4-Aminopyrazolopyrimidine Metabolite That May Contribute to the Hypolipidemic Effects of LY2584702 in Long Evans Diet-Induced Obese Rats. J Pharmacol Exp Ther. 2017 Jul;362(1):108-118. doi: 10.1124/jpet.117.240242. Epub 2017 May 2. PMID: 28465372.
1: Leohr JK, Luffer-Atlas D, Luo MJ, DeBrota DJ, Green C, Mabry TE, Suico JG. Serum Lipid and Protein Changes in Healthy Dyslipidemic Subjects Given a Selective Inhibitor of p70 S6 Kinase-1. J Clin Pharmacol. 2018 Apr;58(4):412-424. doi: 10.1002/jcph.1032. Epub 2017 Nov 26. PubMed PMID: 29178617. 2: Gu X, Fu X, Lu J, Saijilafu, Li B, Luo ZP, Chen J. Pharmacological inhibition of S6K1 impairs self-renewal and osteogenic differentiation of bone marrow stromal cells. J Cell Biochem. 2018 Jan;119(1):1041-1049. doi: 10.1002/jcb.26272. Epub 2017 Aug 28. PubMed PMID: 28853173. 3: Chen B, Yang L, Zhang R, Gan Y, Zhang W, Liu D, Chen H, Tang H. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891. doi: 10.1371/journal.pone.0182891. eCollection 2017. PubMed PMID: 28792981; PubMed Central PMCID: PMC5549961. 4: Estridge TB, Dey AB, Reidy C, Yu X, Zhang Y, Hartley M, Milligan PL, Jin N, Kowala MC, Leohr JK, Fretland AJ, Mabry TE, Luffer-Atlas D, Luo MJ. Identification of 4-Aminopyrazolopyrimidine Metabolite That May Contribute to the Hypolipidemic Effects of LY2584702 in Long Evans Diet-Induced Obese Rats. J Pharmacol Exp Ther. 2017 Jul;362(1):108-118. doi: 10.1124/jpet.117.240242. Epub 2017 May 2. PubMed PMID: 28465372. 5: Archambault AS, Turcotte C, Martin C, Lefebvre JS, Provost V, Laviolette M, Flamand N. Leukotriene B₄ Metabolism and p70S6 Kinase 1 Inhibitors: PF-4708671 but Not LY2584702 Inhibits CYP4F3A and the ω-Oxidation of Leukotriene B₄ In Vitro and In Cellulo. PLoS One. 2017 Jan 9;12(1):e0169804. doi: 10.1371/journal.pone.0169804. eCollection 2017. PubMed PMID: 28068410; PubMed Central PMCID: PMC5222342. 6: Hollebecque A, Houédé N, Cohen EE, Massard C, Italiano A, Westwood P, Bumgardner W, Miller J, Brail LH, Benhadji KA, Soria JC. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours. Eur J Cancer. 2014 Mar;50(5):876-84. doi: 10.1016/j.ejca.2013.12.006. Epub 2014 Jan 20. PubMed PMID: 24456794. 7: Tolcher A, Goldman J, Patnaik A, Papadopoulos KP, Westwood P, Kelly CS, Bumgardner W, Sams L, Geeganage S, Wang T, Capen AR, Huang J, Joseph S, Miller J, Benhadji KA, Brail LH, Rosen LS. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. Eur J Cancer. 2014 Mar;50(5):867-75. doi: 10.1016/j.ejca.2013.11.039. Epub 2014 Jan 15. PubMed PMID: 24440085.