Inhibitor Expert (Inhibitors, Compound Libraries)

Print

LY2584702

Technical Data

Molecular Weight 445.42 Storage powder
Formula

C21H19F4N7

in solvent
CAS No. 1082949-67-4 Synonyms N/A
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
Solubility (25°C) * In vitro DMSO 1 mg/mL warmed (2.24 mM)
Water Insoluble
Ethanol Insoluble
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Biological Activity

Description LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
Targets
p70S6K [1]
4 nM
In vitro In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM. [1] LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus. [2]
In vivo LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models. [1]
Features  

Protocol (Only for Reference)

Animal Study:

[1]

Animal Models U87MG glioblastoma and HCT116 colon carcinoma xenograft models
Formulation --
Dosages 12.5 mg/kg BID
Administration --
 

References:

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2016, 7(25):38451-38466]

Murine DCs were pretreated with PBS or kinase inhibitors (10 μmol/l) wortmanni LY2584702 2 h prior to nicotine (10−7 mol/l) 12~15 h stimulation. MR expression was determined via western blot analyses (C, F). β-actin was used as an internal control.

Data from [Data independently produced by , , J Immunol, 2016, 197(9):3545-3553]

(A) Flow cytometry for TNF-α and IL-12 p40 intracellular expression and ELISA assays for IL-12p70 and IL-23 in supernatants of untreated or treated cells after 24 h. Results were expressed as pictograms per milliliter (± SD) from four independent experiments, each performed in triplicate. *p < 0.05 versus IFN-γ, **p < 0.01 versus IFN-γ.

LY2584702 has been referenced in publications.

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

* Return Policy

Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.

Toll Free:
(877) 796-6397
-- USA and Canada only --
Fax:
+1-713-796-9816
Orders:
+1-832-582-8158
sales@selleckchem.com
Tech Support:
+1-832-582-8158 Ext:3
tech@selleckchem.com
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
Website:
www.selleckchem.com