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.
CAS Number: 957054-30-7
Molecular Weight: 513.64
Related CAS Number:
Chemical Name: 4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
GDC-0941 was used at 1-10 µM in vitro and in cellular assays.
GDC-0941 was orally dosed to mice at 75-150 mg/kg once per day for two weeks.
- Folkes AJ, et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer.(2008) J. Med. Chem. 51(18), 5522-32.
- Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. (2009) Mol. Cancer Ther. 8(7), 1725-38.
- Zheng L, et al. GDC-0941 sensitizes breast cancer to ABT-737 in vitro and in vivo through promoting the degradation of Mcl-1.(2011) Cancer Lett. 309(1):27-36.
- Haagensen EJ, et al. The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. (2012) Br J Cancer. 106(8):1386-94.
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