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Pictilisib

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]

Product Name Alternative

GDC-0941

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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.html

Purity

99.80

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ

Citation 01

Anticancer Res. 2025 Apr;45 (4) :1355-1366.|Arab J Gastroenterol. 2025 Feb;26 (1) :104-111.|Biochem Biophys Res Commun. 2025 Jun 12:776:152203.|Biochem J. 2022 Oct 14;479 (19) :2131-2151.|Bioorg Med Chem Lett. 2012 Mar 1;22 (5) :1874-8. |bioRxiv. 2020 Mar.|bioRxiv. 2025 Jul 23:2025.07.18.665614.|bioRxiv. 2025 May 16.|bioRxiv. 2025 Sep 20:2025.09.17.676669.|Br J Cancer. 2021 Apr;124 (9) :1581-1591.|Cancer Discov. 2012 May;2 (5) :425-33.|Cancer Med. 2025 Sep;14 (18) :e71227.|Cancer Res. 2014 Jan 1;74 (1) :15-23.|Cancer Res. 2024 Sep 16;84 (18) :2985-3003.|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.|Cell. 2025 May 29;188 (11) :3065-3080.e21. |Chem Biodivers. 2025 Apr;22 (4) :e202403291.|Debreceni egyettemmolekularis orvostudomany. 2024 Dec.|Free Radic Biol Med. 2025 Oct 30:242:275-287.|Gastroenterology. 2025 Oct 27:S0016-5085 (25) 05903-7.|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. 2023 Jan 17;133 (2) :e153470.|J Pharm Anal. 2025 May;15 (5) :101092.|J Surg Res. 2023 Feb:282:137-146.|J Virol. 2025 Aug 25:e0022125.|Lipids Health Dis. 2024 Sep 4;23 (1) :282.|MedComm (2020) . 2024 Aug 12;5 (8) :e684.|Mol Cell. 2025 Aug 7;85 (15) :2973-2987.e6.|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. 2025 Mar;21 (3) :432-442.|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;27 (1) :18.|Oncol Rep. 2023 Jul;50 (1) :131.|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 Signal. 2025 Sep 2;18 (902) :eadw3231.|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. 2022 Jan;15 (1) :101260.|Cell Rep. 2020 Sep 29;32 (13) :108196.

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