GDC-0941 dimethanesulfonate

Research use only, not for human use.

A potent, selective, orally bioavailable inhibitor of class I PI3Ks with IC50 of 3/33/3/75 nM for p110α/β/γ/δ, respectively.

A potent, selective, orally bioavailable inhibitor of class I PI3Ks with IC50 of 3/33/3/75 nM for p110α/β/γ/δ, respectively; shows similar activity for mutant p110α E545K and H1047R (IC50=3 nM), weak or little activity for C2α, Vps34, DNA-PK, and mTOR (IC50>500 nM); inhibits Akt (Ser473) phosphorylation in U87MG, PC3, and MDA-MB-361 cells with IC50s of 46, 37, and 28 nM, respectively, and respective GI50 is 0.95, 0.28, and 0.72 uM; exhibits tumor growth inhibition in U87MG human glioblastoma xenografts.Breast Cancer Phase 2 Clinical

Pictilisib dimethanesulfonate

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

Breast Cancer

957054-33-0

705.85

C25H35N7O9S4

>98% (HPLC)

10 mM in DMSO

CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6.CS(=O)(=O)O.CS(=O)(=O)O

Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-, methanesulfonate (1:2)

(-20℃)

With Ice Pack

≥ 2 years