ETP-46321

Research use only, not for human use.

ETP-46321 is a potent, selective, orally bioavailable dual PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM.

ETP-46321 is a potent, selective, orally bioavailable dual PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM, weakly inhibits p110β and p110γ with IC50 of 170 and 179 nM; shows highly selectivity versus mTOR and 288 representative kinases, also potently inhibits mutants PI3K α E542K, E545K, and H1047R with IC50 of ~2 nM, inhibits phosphorylation of AKT Ser473 in the U2OS cell line with IC50 of 8.3 nM; shows significant tumor growth inhibition and reduction of the tumor metabolic activity in a lung tumor mouse model driven by a K-RasG12V oncogenic mutation.

ETP 46321;ETP46321

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

——

1252594-99-2

473.55

C20H27N9O3S

>98% (HPLC)

DMSO: ≥ 33 mg/mL

NC1=NC=C(C2=CN3C(C(N4CCOCC4)=N2)=NC(CN5CCN(S(=O)(C)=O)CC5)=C3)C=N1

2-Pyrimidinamine, 5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-8-(4-morpholinyl)imidazo[1,2-a]pyrazin-6-yl]-

(-20℃)

With Ice Pack

≥ 2 years