GDC-0941

• CAT Number: I005672
• CAS Number: 957054-30-7
• Molecular Formula: C₂₃H₂₇N₇O₃S₂
• Molecular Weight: 513.64
• Purity: ≥95%
• Synonyms: GDC0941；GDC 0941
• Target: PI3K
• Solubility: DMSO: ≥ 29 mg/mL
• Storage: 3 years -20C powder
• IC50: 3 nM
• IUPAC Name: 4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine
• InChI: InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)
• InChIKey: LHNIIDJUOCFXAP-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6

GDC-0941（Cat No.:I005672）is a potent and selective inhibitor of class I phosphoinositide 3-kinase (PI3K), targeting the PI3K/Akt/mTOR signaling pathway crucial for cell growth, survival, and metabolism. By inhibiting PI3K, GDC-0941 effectively reduces cancer cell proliferation, induces apoptosis, and interferes with tumor progression. It has demonstrated anticancer activity in preclinical and clinical trials, showing potential for treating solid tumors, including breast and lung cancers. GDC-0941 is a valuable research tool for investigating PI3K-targeted cancer therapies, particularly for tumors with aberrant PI3K pathway activation.

Reference

[1]. Folkes, Adrian J.; Ahmadi, Khatereh; 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 .Journal of Medicinal Chemistry (2008) Volume: 51, Issue: 18, Publisher: American Chemical Society, Pages: 5522-5532 


[2]. Wallin JJ, Guan J, Prior WW, Lee LB, Berry L, Belmont LD, Koeppen H, Belvin M, Friedman LS, Sampath D.GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18(14):3901-11. Epub 2012 May 14. 


[3]. Wullschleger S, García-Martínez JM, Duce SL.Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.Anticancer Res. 2012 Feb;32(2):415-20. 


[4]. Zou ZQ, Zhang LN, Wang F, Bellenger J, Shen YZ, Zhang XH.The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5(2):503-8. 


[5]. Burrows N, Babur M, Resch J, Ridsdale S, Mejin M, Rowling EJ, Brabant G, Williams KJ.GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct 12.