GDC-0941 --- PI3K Inhibitor
| Overview | |
| Catalog # | bs-60111c-5-mg-solid |
| Product Name | GDC-0941 --- PI3K Inhibitor |
| Specifications | |
| Storage Buffer | Powder |
| Storage Condition | Store in dry, dark place at -20C for 1 year. |
| Target | |
| Product Information | Molecular Weight: 513.64 Formula: C23 H27 N7 O3 S2 CAS Number: 957054-30-7 InChi Key: LHNIIDJUOCFXAP-UHFFFAOYSA-N InChi: InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27) Smiles: CS(=O)(=O)N1CCN(CC2=CC3N=C(N=C(C=3S2)N2CCOCC2)C2C=CC=C3NN=CC=23)CC1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
| Description | GDC-0941 is a highly potent, selective and orally bioavailable class-I PI3K kinase inhibitor. Its IC50 for PI3K p110 α, β, δ and γ 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 μM, 0.14 μM, 0.28 μM, and 0.72 μM, 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. |
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