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Background Information:
GDC-0941 is a potent and selective inhibitor of class I PI3 kinase (PI3K) with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR, respectively, exhibiting excellent pharmacokinetic properties in all animal models.
Reference:
1. Salphati L, Lee LB, Pang J, Plise EG, Zhang X. Role of P-glycoprotein and Breast Cancer Resistance Protein-1 in the Brain Penetration and Brain Pharmacodynamic Activity of the Novel PI3K Inhibitor GDC-0941. Drug Metab Dispos. 2010 Jun 3. [Epub ahead of print] PubMed PMID: 20522663.
2. Napper AD. Society for biomolecular sciences - 16th annual conference & exhibition - advancing the science of drug discovery. IDrugs. 2010 Jun;13(6):372-5.
3. O'Brien C, Wallin JJ, Sampath D, Guhathakurta D, Savage H, Punnoose EA, Guan J, Berry L, Prior WW, Amler LC, Belvin M, Friedman L, Lackner M. Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3' Kinase Inhibitor GDC-0941 In Breast Cancer Preclinical Models. Clin Cancer Res. 2010 May 7. [Epub ahead of print] PubMed PMID: 20453058.
APIM050150: GDC-0941 (FREE BASE)
CAS No.: 957054-30-7.
Molecular Formula: C23H27N7O3S2.
Molecular Weight: 513.63.
Purity: >99% (HPLC at 214 and 254 nm).
QC: LC/MS, 1HNMR, HPLC.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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