GDC-0941 Dimethanesulfonate

• CAT Number: I005673
• CAS Number: 957054-33-0
• Molecular Formula: C₂₅H₃₅N₇O₉S₄
• Molecular Weight: 705.85
• Purity: ≥95%
• Synonyms: 4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine;methanesulfonic acid
• Target: PI3K
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 3 nM
• InChI: InChI=1S/C23H27N7O3S2.2CH4O3S/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;2*1-5(2,3)4/h2-4,13-14H,5-12,15H2,1H3,(H,24,27);2*1H3,(H,2,3,4)
• InChIKey: RFRIKACSFOTIMU-UHFFFAOYSA-N
• SMILES: CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6.CS(=O)(=O)O.CS(=O)(=O)O

GDC-0941 Dimethanesulfonate（Cat No.:I005673）is a potent and selective inhibitor of class I phosphoinositide 3-kinase (PI3K), primarily targeting the PI3K/Akt/mTOR signaling pathway. This pathway plays a crucial role in regulating cell growth, proliferation, and survival, making GDC-0941 a valuable compound for cancer research. It has demonstrated significant antitumor activity in various preclinical models, particularly in breast and prostate cancers. GDC-0941 is also being explored in combination therapies to enhance its efficacy and overcome resistance mechanisms in targeted cancer treatments, contributing to advancements in precision oncology.

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 .J Med Chem. 2008 Sep 25;51(18):5522-32.


[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.