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GDC-0941,  PI3K Inhibitor

GDC-0941, PI3K Inhibitor

$79.00
A highly potent, selective and orally bioavailable class-I PI3K kinase inhibitor.
Catalog No. Unit Price Qty
M60111-5s 5mg solid $79.00
M60111-50s 50mg solid $350.00

Details

Product Information
Molecular Weight: 513.64
Formula: C23H27N7O3S2
Purity: ≥98%
CAS#: 957054-30-7
Solubility: DMSO up to 100 mM
Chemical Name: 4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

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.

 

How to Use:

  • In vitro: GDC-0941 was used at 1-10 µM in vitro and in cellular assays. 
  • In vivo: GDC-0941 was orally dosed to mice at 75-150 mg/kg once per day for two weeks.

 

Reference:

  • 1. 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.
  • 2. 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.
  • 3.  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.  
  • 4.  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. 
  •  

  • GDC-0941_spec.pdf
  • GDC-0941_MSDS.pdf


 

Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 513.64
Formula: C23H27N7O3S2
Purity: ≥98%
CAS#: 957054-30-7
Solubility: DMSO up to 100 mM
Chemical Name: 4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

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.

 

How to Use:

  • In vitro: GDC-0941 was used at 1-10 µM in vitro and in cellular assays. 
  • In vivo: GDC-0941 was orally dosed to mice at 75-150 mg/kg once per day for two weeks.

 

Reference:

  • 1. 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.
  • 2. 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.
  • 3.  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.  
  • 4.  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. 
  •  

  • GDC-0941_spec.pdf
  • GDC-0941_MSDS.pdf


 

Products are for research use only. Not for human use.

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