Pictilisib (dimethanesulfonate)

Pictilisib (dimethanesulfonate)

• CAS Number: 957054-33-0
• UNSPSC Description: Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
• Target Antigen: Apoptosis; Autophagy; PI3K
• Type: Reference compound
• Related Pathways: Apoptosis;Autophagy;PI3K/Akt/mTOR
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/GDC-0941-dimethanesulfonate.html
• Purity: 99.72
• Solubility: DMSO : 7.14 mg/mL (ultrasonic;warming)|H2O : 7.14 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: O=S(N1CCN(CC1)CC2=CC3=C(S2)C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)(C)=O.O=S(O)(C)=O.O=S(O)(C)=O
• Molecular Weight: 705.85
• 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.Cell Rep. 2020 Sep 29;32(13):108196.|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.|Cancer Res. 2024 Jun 17.|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.|Debreceni egyettemmolekularis orvostudomany. 2024 Dec.|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 Pharm Anal. 2024 Aug 29.|J Surg Res. 2022 Oct 20;282:137-146.|Lipids Health Dis. 2024 Sep 4;23(1):282.|MedComm (2020). 2024 Aug 12;5(8):e684.|Molecules. 2019 Apr 1;24(7):1260.|Molecules. 2020 Apr 23;25(8):1980.|Nat Biomed Eng. 2018 Aug;2(8):578-588.|Nat Cancer. 2024 Mar;5(3):433-447.|Nat Chem Biol. 2017 Jan;13(1):38-45.|Nat Chem Biol. 2024 Oct 31.|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. US20210236501A1.|Patent. US20220313694A1.|Research Square Preprint. 2024 Nov 26.|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.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Phase 2