LY2584702 Tosylate - CAS 1082949-68-5
Catalog number:
1082949-68-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H27F4N7O3S
Molecular Weight:
617.62
COA:
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Targets:
Ribosomal S6 Kinase (RSK)
Description:
LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
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Purity:
>98%
Related CAS:
1082949-67-4 (Free base)
Appearance:
White to off-white solid powder
Synonyms:
4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine 4-methylbenzenesulfonate; LY2584702; LY 2584702; LY-2584702; LYS6K2
MSDS:
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InChIKey:
HDYUXDNMHBQKAU-UHFFFAOYSA-N
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)
Canonical SMILES:
CN1C=C(C2=CC=C(F)C(C(F)(F)F)=C2)N=C1C3CCN(C4=C5C(NN=C5)=NC=N4)CC3.OS(=O)(C6=CC=C(C)C=C6)=O
1.A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours.
Tolcher A1, Goldman J2, Patnaik A1, Papadopoulos KP1, Westwood P3, Kelly CS4, Bumgardner W4, Sams L4, Geeganage S4, Wang T4, Capen AR4, Huang J4, Joseph S4, Miller J4, Benhadji KA4, Brail LH4, Rosen LS5. Eur J Cancer. 2014 Mar;50(5):867-75. doi: 10.1016/j.ejca.2013.11.039. Epub 2014 Jan 15.
BACKGROUND: 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 preclinical analysis.
2.A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.
Hollebecque A1, Houédé N2, Cohen EE3, Massard C1, Italiano A2, Westwood P4, Bumgardner W5, Miller J5, Brail LH5, Benhadji KA5, Soria JC6. Eur J Cancer. 2014 Mar;50(5):876-84. doi: 10.1016/j.ejca.2013.12.006. Epub 2014 Jan 20.
BACKGROUND: LY2584702 tosylate (hereafter referred to as LY2584702) is an oral, selective ATP competitive inhibitor of p70 S6 kinase. Preclinical studies with LY2584702 demonstrated significant synergistic activity with erlotinib and everolimus. The primary objective was to determine a phase II dose and schedule. Secondary objectives included evaluation of safety, toxicity and pharmacokinetics of LY2584702 in combination with erlotinib or everolimus.
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CAS 1082949-68-5 LY2584702 Tosylate

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