GDC-0980

Research use only, not for human use.

GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM.

GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM; displays remarkably selective for several other members of the closely related PIKK family kinases, including C2alpha, C2beta, VPS34 I, PI4Kalpha, PI4Kbeta and DNA-PK; potently inhibits signal transduction downstream of both PI3K and mTOR, reduces viability in multiple cancer cell lines by cell-cycle inhibition and induction of apoptosis (prostate IC50<200 nM, NSCLC lines <200 nM); potently inhibits tumor growth in xenograft models with activated PI3K, loss of LKB1 or PTEN.Breast Cancer Phase 2 Clinical

Apitolisib;GNE 390;GDC0980;RG 7422

PI3K/Akt/mTOR signaling

PI3K

mTOR;p110α;p110β;p110γ;p110δ

Cancer

Breast Cancer

1032754-93-0

498.60

C23H30N8O3S

>98% (HPLC)

10 mM in DMSO

C[C@H](O)C(N1CCN(CC2=C(C)C3=NC(C4=CN=C(N)N=C4)=NC(N5CCOCC5)=C3S2)CC1)=O

1-Propanone, 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-, (2S)-

(-20℃)

With Ice Pack

≥ 2 years