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LY2584702

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LY2584702 Basic information

Product Name:
LY2584702
Synonyms:
  • LY2584702
  • LY-2584702 (free base)
  • LY2584702 TsOH
  • 4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methyl-imidazol-2-yl]-1-piperidyl]-1H-pyrazolo[3,4-d]pyrimidine LY2584702
  • 4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine
  • 4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methylimidazol-2-yl]piperidin-1-yl]-1H-pyrazolo
  • LY2584702 BASE
  • LY-2584702 free base (LY2584702)
CAS:
1082949-67-4
MF:
C21H19F4N7
MW:
445.42
Product Categories:
  • Inhibitors
Mol File:
1082949-67-4.mol
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LY2584702 Chemical Properties

storage temp. 
RT (des.)
solubility 
Soluble in DMSO (up to 1 mg/ml) or in DMF (up to 3 mg/ml).
form 
solid
color 
Yellow
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months.
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Safety Information

HS Code 
2933998090
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LY2584702 Usage And Synthesis

Description

LYS6K2 (1082949-67-4) is a selective inhibitor of the p70 ribosomal S6 kinase (S6K).1 Blocks the phosphorylation of S6 at concentrations as low as 0.1-0.3 μM with no activity at GSK3β and Erk1/2 at 10 μM.2?LYS6K2 is a useful tool to dissect insulin receptor signaling pathways and was employed to show that the action of mTORC1 on SREB P-1c expression is not mediated by S6K.2?Cell permeable.

Uses

LY 2584702 is an orally available inhibitor of p70S6K signalling and potential antineoplastic activity. Used in combination with Erlotinib or Everolimus as an anti-tumor treatment.

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)

References

[1] TIM R. FENTON  Ivan T G. Functions and regulation of the 70 kDa ribosomal S6 kinases[J]. International Journal of Biochemistry & Cell Biology, 2011, 43 1: Pages 47-59. DOI:10.1016/j.biocel.2010.09.018
[2] SHIJIE LI  Joseph L G  Michael S Brown. Bifurcation of insulin signaling pathway in rat liver: mTORC1 required for stimulation of lipogenesis, but not inhibition of gluconeogenesis.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2010, 107 8: 3441-3446. DOI:10.1073/pnas.0914798107

LY2584702Supplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
Haoyuan Chemexpress Co., Ltd.
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021-58950125
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info@chemexpress.com
CEG Chemical Science&Technology Co., Ltd.
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Mobile:13665161512
Suzhou yacoo science co.,Ltd
Tel
0512-87182056 18013166090
Email
lingling.qi@yacoo.com.cn
AdooQ Bioscience CHINA
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025-58849295 18951903616;
Email
info@adooq.cn
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