product name LY2584702
Description: LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. In both HCT116 colon carcinoma and U87MG glioblastoma xenograft models, LY2584702 at levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID exhibited significant efficacy. Treatment patients with advanced solid tumours with LY2584702 orally on a 28-day cycle, the maximum tolerated dose (MTD) was 75 mg BID (twice-daily) or 100 mg QD (once-daily).
References: Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.
445.42
Formula
C21H19F4N7
CAS No.
1082949-67-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 1 mg/mL (2.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
In Vitro |
In vitro activity: In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM. LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus. Kinase Assay: Cell Assay: |
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In Vivo | LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models. |
Animal model | |
Formulation & Dosage | |
References | Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84. |