Download Files:
Pictilisib
$66 – $277
Products Details
Product Description
– 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).
Web ID
– HY-50094
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C23H27N7O3S2
Citations
– Biochem J. 2022 Oct 14;479(19):2131-2151.|Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. |bioRxiv. 2020 Mar.|Br J Cancer. 2021 Mar 15.|Cancer Discov. 2012 May;2(5):425-33.|Cancer Res. 2014 Jan 1;74(1):15-23.|Cancers. 2020 Jul 16;12(7):1918.|Cell Biosci. 2022 Aug 21;12(1):135.|Cell Cycle. 2019 Jul;18(13):1513-1522. |Cell Metab. 2012 Mar 7;15(3):382-94.|Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.|Cell Rep. 2023 May 29;42(6):112570.|Cell Syst. 2020 Jan 22;10(1):66-81.e11.|Cell. 2023 Jun 22;186(13):2929-2949.e20.|Harvard Medical School LINCS LIBRARY|Int J Clin Exp Pathol. 2017;10(3):3033-3042.|Int J Oncol. 2017 Sep;51(3):823-831.|J Cell Biol. 2020 Dec 7;219(12):e202001031.|J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246.|J Clin Invest. 2022 Nov 22;e153470.|J Surg Res. 2022 Oct 20;282:137-146.|Molecules. 2019 Apr 1;24(7):1260.|Molecules. 2020 Apr 23;25(8):1980.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Nat Chem Biol. 2017 Jan;13(1):38-45.|Nat Commun. 2015 Oct 7;6:8501. |Nat Commun. 2016 Feb 2;7:10438.|Nature. 2018 Aug;560(7719):499-503.|Oncogene. 2016 Jun 9;35(23):2961-70. |Oncol Lett. 2023 Nov 15.|Oncol Rep. 2023 May 9.|Oncotarget. 2016 Aug 16;7(33):53515-53525.|Oncotarget. 2016 May 31;7(22):32641-51. |Patent. US20220313694A1.|Sci Rep. 2021 Jan 11;11(1):291.|Sci Signal. 2021 Dec 21;14(714):eabj0057.|Sci Transl Med. 2013 Jul 31;5(196):196ra99.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Tierärztliche Hochschule Hannover. 2021 Jul.|Transl Oncol. January 2022, 101260.|Cell Rep. 2020 Sep 29;32(13):108196.
References
– [1]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.|[2]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.|[3]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.|[4]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.|[5]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.|[6]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|[7]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.
CAS Number
– 957054-30-7
Molecular Weight
– 513.64
Compound Purity
– 99.80
SMILES
– CS(N1CCN(CC2=CC3=C(C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)S2)CC1)(=O)=O
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Apoptosis;Autophagy;PI3K
Isoform
– PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ
Pathway
– Apoptosis;Autophagy;PI3K/Akt/mTOR
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
