| Identification | Back Directory | [Name]
LY-2584702 (hydrochloride) | [CAS]
1082948-81-9 | [Synonyms]
LY2584702 HCl
LY-2584702 (hydrochloride)
LY-2584702 hydrochloride
(LY2584702)
LY 2584702 hydrochloride,LY2584702 hydrochloride
4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine hydrochloride (1:1) | [Molecular Formula]
C21H20ClF4N7 | [MDL Number]
MFCD30478836 | [MOL File]
1082948-81-9.mol | [Molecular Weight]
481.88 |
| Hazard Information | Back Directory | [Uses]
LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM. | [in vivo]
LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model[1]. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3[2]. | [IC 50]
p70S6K: 4 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75. DOI:10.1016/j.ejca.2013.11.039
[2] Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50. DOI:10.1158/0008-5472.CAN-13-2961
[3] Chen B, et al. 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 |
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