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GDC-0941 | Class I PI3K kinase inhibitor

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  • GDC-0941, 400x400px, png
Price:
$109.00
Catalog #:
C4321-5
Quantity:


Product Description

GDC-0941 is a highly potent and selective class I PI3K kinase inhibitor under development. Its IC50 values for for PI3K p110 α, β, δ and γ isoforms are 3nM, 33nM, 3nM, 75nM, and for DNA-PK and mTOR are 1230nM and 580nM. It is now in phase I clinical trials targeting several advanced or metastatic solid tumors.


Technical information:

Chemical Formula:   C23H27N7O3S2
CAS #:   957054-30-7
Molecular Weight:   513.64
Purity:   >98%
Appearance:   White solid
Chemical Name:   4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
Solubility:   Up to 100 mM in DMSO

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. AJ Folkes 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. J. Med. Chem. 2008, 51(18), 5522-32.
2. FI Raynaud 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. Mol. Cancer Ther. 2009, 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.Cancer Lett. 2011;309(1):27-36.

Other Information:

Product Specification (pdf)
MSDS (pdf)

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