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SML2892

Sigma-Aldrich

LY2584702 tosylate

≥98% (HPLC)

Synonym(s):

4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine, 4-methylbenzenesulfonate (1:1), LY 2584702 tosylate, LY 2779964, LY-2584702 tosylate, LY-2779964, LY2779964, LYS6K2 tosylate

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About This Item

Empirical Formula (Hill Notation):
C21H19F4N7 · C7H8O3S
CAS Number:
1082949-68-5
Molecular Weight:
617.62
MDL number:
MFCD29054739
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

InChI

1S/C21H19F4N7.C7H8O3S/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;1-6-2-4-7(5-3-6)11(8,9)10/h2-3,8-12H,4-7H2,1H3,(H,26,27,28,30);2-5H,1H3,(H,8,9,10)

InChI key

HDYUXDNMHBQKAU-UHFFFAOYSA-N

Biochem/physiol Actions

LY2584702 is an orally active, ATP-competitive, potent and selective ribosomal protein S6 kinase (p70 S6 kinase, p70S6K, S6K1) inhibitor (IC50 = 4 nM; selective over 83 other kinases and 45 cell surface markers). LY2584702 inhibits HCT116 cellular S6 phosphorylation (IC50 0.1-0.24 μM) and shows anti-tumor efficacy in U87MG glioblastoma and HCT116 colon carcinoma xenograft models in vivo (2.5 mg/kg bid. po.).

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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PI3K is one of the most frequently mutated genes in cancers and has been the target of numerous anticancer therapies. With the additional development of therapeutics that mobilize the immune system, such as Abs with effector functions, bispecific Abs, and
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BRAF and MEK inhibitors have shown remarkable clinical efficacy in BRAF-mutant melanoma; however, most patients develop resistance, which limits the clinical benefit of these agents. In this study, we found that the human melanoma cell clones, A375-DR and A375-TR, with
Anthony Tolcher et al.
European journal of cancer (Oxford, England : 1990), 50(5), 867-875 (2014-01-21)
LY2584702 tosylate (hereafter referred to as LY2584702) is a potent, highly selective adenosine triphosphate (ATP) competitive inhibitor against p70 S6 kinase, a downstream component of the phosphatidylinositol-3-kinase signalling pathway which regulates cell proliferation and survival. LY2584702 exhibited anti-tumour activity in
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