Pictilisib dimethanesulfonate Inhibitor

Pictilisib dimethanesulfonate is a potent inhibitor of PI3Kalpha/delta with IC50 of 3nM, with modest selectivity against p110beta (11-fold) and p110gamma (25-fold).

Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18(14):3901-1Epub 2012 May 14.
Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 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.
Folkes AJ, 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.
Folkes AJ, 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.
Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatment, in PTEN-deficient mice lymphoma. Anticancer Res. 2012 Feb;32(2):415-20.
Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatment, in PTEN-deficient mice lymphoma. Anticancer Res. 2012 Feb;32(2):415-20.
Zou ZQ, et al. 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.
Zou ZQ, et al. 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.
Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1alpha (HIF-1alpha) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct
Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1alpha (HIF-1alpha) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct

Small volumes of Pictilisib dimethanesulfonate, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5753177 is an inhibitor targeting Pictilisib dimethanesulfonate.