GDC0941

5 mg

Cat. No.: 78-S14

$99.00

GDC0941 is a phosphatidylinositol 3-kinase (P13K) inhibitor. GDC-0941 inhibits the activity of recombinant PI3K in vitro with IC50’s of 0.003 µM (P110α), 0.033 µM (P110β), 0.003 µM (P110δ), 0.075 µM (P110γ), 0.58 µM (mTOR) and 1.23 µM (DNA-PK).

 

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TECHNICAL INFORMATION

Other Names: 2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-thieno[3,2- d]pyrimidine

Chemical Formula: C23H27N7O3S2

CAS Number: 957054-30-7

Molecular Weight: 513.64

Purity:  >98%

Appearance:  a crystalline solid  

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO at 66mg/ml. If precipitate is observed,  vortex for 5 minutes. For most cells, the maximum tolerance to DMSO is less than 0.5%. 

References

Folkes et al. (2008) 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. J Med Chem. 51(18):5522-32.

Junttila et al. (2009) Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941. Cancer Cell. 15(5):429-40.

Raynaud et al. (2009) 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. Mol Cancer Ther. 8(7):1725-38.

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