LY2584702

Alias: LYS6K2; LY 2584702; LY-2584702; LY2584702; LYS 6K2; LYS-6K2

Cat No.:V0240 Purity: ≥98%

COA Product Data Instructions for use SDS

LY2584702 is a novel, selective, orally bioavailable, and ATP-competitive inhibitor of p70S6K (ribosomal p70 S6 kinase) with potential antitumor activity.

LY2584702 Chemical Structure CAS No.: 1082949-67-4
Product category: S6 kinase

This product is for research use only, not for human use. We do not sell to patients.

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

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.

Biological Activity I Assay Protocols (From Reference)

Targets	p70S6K (IC50 = 4 nM)
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]
ln Vivo	In the xenograft models of U87MG glioblastoma and HCT116 colon carcinoma, LY2584702 (12.5 mg/kg BID) exhibits significant antitumor efficacy. [1]
Enzyme Assay	LY2584702 Tosylate (also known as LYS6K2) is a novel, selective, orally bioavailable, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
Cell Assay	Cells were treated with indicated concentration of drug for 24 h.
Animal Protocol	U87MG glioblastoma and HCT116 colon carcinoma xenograft models 12.5 mg/kg BID
References	[1]. Eur J Cancer . 2014 Mar;50(5):867-75. [2]. Eur J Cancer . 2014 Mar;50(5):876-84./ [3]. Transl Psychiatry. 2022 May 4;12(1):184.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C21H19F4N7
Molecular Weight	445.4256
Exact Mass	445.1638
Elemental Analysis	C, 56.63; H, 4.30; F, 17.06; N, 22.01
CAS #	1082949-67-4
Related CAS #	LY-2584702 tosylate salt;1082949-68-5;LY-2584702 hydrochloride;1082948-81-9
Appearance	Solid powder
SMILES	CN1C=C(N=C1C2CCN(CC2)C3=NC=NC4=C3C=NN4)C5=CC(=C(C=C5)F)C(F)(F)F
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)
Chemical Name	4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methylimidazol-2-yl]piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine
Synonyms	LYS6K2; LY 2584702; LY-2584702; LY2584702; LYS 6K2; LYS-6K2
HS Tariff Code	2934.99.03.00
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)

Solubility Data

Solubility (In Vitro)	DMSO: ~1 mg/mL (~2.2 mM) Water: <1 mg/mL Ethanol: <1 mg/mL

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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

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

Biological Data

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.
Proliferation alteration of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702 (CCK-8 analysis).PLoS One.2017 Aug 9;12(8):e0182891.
Cell cycle distribution of NSCLC cell lines with RPS6KB1 dephosphorylation by LY2584702.PLoS One.2017 Aug 9;12(8):e0182891.