Pictilisib (Standard)

Pictilisib (Standard) is the analytical standard of Pictilisib. This product is intended for research and analytical applications. Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold) .

Product Specifications

CAS Number

[957054-30-7]

UNSPSC

12352100

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; PI3K; Reference Standards

Related Pathways

Apoptosis; Autophagy; Others; PI3K/Akt/mTOR

Field of Research

Cancer

Purity

98.06

Smiles

CS(N1CCN(CC2=CC3=C(C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)S2)CC1)(=O)=O

Molecular Formula

C23H27N7O3S2

Molecular Weight

513.64

Precautions

H302, H315, H319, H335

References & Citations

[1]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.|[2]Wullschleger S, et al. 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.|[3]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.|[4]Burrows N, et al. 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|[5]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.|[6]Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2 (5) :425-33.|[7]Cheng H, et al. A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. Cancer Res. 2014 Jan 1;74 (1) :15-23.