GDC-0941 --- PI3K Inhibitor [957054-30-7] [957054-30-7]

Bioss

GDC-0941 --- PI3K Inhibitor [957054-30-7] [957054-30-7]

16

957054-30-7

Research Use Only

Unconjugated

98 - 98.0

C23 H27 N7 O3 S2

513.64

GDC-0941 is a highly potent, selective and orally bioavailable class-I PI3K kinase inhibitor. Its IC50 for PI3K p110 alpha, beta, delta and gamma isoforms are 3 nM, 33 nM, 3 nM, and 75 nM, respectively; and its IC50 for DNA-PK and mTOR are 1230 nM and 580 nM. It potently inhibits the phosphorylation of Akt in U87MG, PC3, and MDA-MB-361 cells with IC50 of 46 nM, 37 nM, and 28 nM, respectively. It also inhibits the proliferation of U87MG, A2780, PC3, and MDA-MB-361 cells with IC50 of 0.95 microM, 0.14 microM, 0.28 microM, and 0.72 microM, respectively. GDC-0941 inhibits tumor cell proliferation, induces apoptosis and suppresses centroblast population. It is now in Phase I clinical trials targeting several advanced or metastatic solid tumors.

CS(=O)(=O)N1CCN(CC2=CC3N=C(N=C(C=3S2)N2CCOCC2)C2C=CC=C3NN=CC=23)CC1

-20°C

12161509