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Details

Stereochemistry ACHIRAL
Molecular Formula C21H19F4N7
Molecular Weight 445.4161
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LY-2584702

SMILES

CN1C=C(N=C1C2CCN(CC2)C3=C4C=NNC4=NC=N3)C5=CC=C(F)C(=C5)C(F)(F)F

InChI

InChIKey=FYXRSVDHGLUMHB-UHFFFAOYSA-N
InChI=1S/C21H19F4N7/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/h2-3,8-12H,4-7H2,1H3,(H,26,27,28,30)

HIDE SMILES / InChI

Description

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 underwent clinical trials against solid tumors both as a monotherapy and in combination with erlotinib or everolimus. No responses were observed for treatment as a single agent. LY2584702 was not well tolerated when administered with erlotinib, therefore this combination is not feasible. The combination with everolimus was better tolerated but yielded very limited clinical benefit.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
841.58 ng/mL
50 mg 2 times / day steady-state, oral
LY-2584702 blood
Homo sapiens
1843 ng/mL
300 mg 1 times / day single, oral
LY-2584702 blood
Homo sapiens
1518.04 ng/mL
100 mg 1 times / day steady-state, oral
LY-2584702 blood
Homo sapiens
2529.26 ng/mL
100 mg 2 times / day steady-state, oral
LY-2584702 blood
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
4470.57 ng × h/mL
50 mg 2 times / day steady-state, oral
LY-2584702 blood
Homo sapiens
30897 ng × h/mL
300 mg 1 times / day single, oral
LY-2584702 blood
Homo sapiens
6106.05 ng × h/mL
100 mg 1 times / day steady-state, oral
LY-2584702 blood
Homo sapiens
13718.79 ng × h/mL
100 mg 2 times / day steady-state, oral
LY-2584702 blood
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
3.42 h
300 mg 1 times / day single, oral
LY-2584702 blood
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
LY2584702 tosylate was administered orally in a dose-escalating regime starting with 25 mg QD. The MTD was determined to be 75 mg BID or 100 mg QD.
Route of Administration: Oral
In Vitro Use Guide
Unknown