LY2584702 free base

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MedKoo CAT#: 206867

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

Description: 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
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: 445.4256
Elemental Analysis: C, 56.63; H, 4.30; F, 17.06; N, 22.01

Price and Availability

Size Price Availability Quantity
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
200.0mg USD 1250.0 2 Weeks
500.0mg USD 2850.0 2 Weeks
1.0g USD 3850.0 2 Weeks
2.0g USD 6450.0 2 Weeks
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Related CAS #: 1082949-68-5 (tosylate)   1082949-67-4 (free base)    

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 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

Preparing Stock Solutions

The following data is based on the product molecular weight 445.4256 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

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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.