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Pictilisib (dimethanesulfonate)

Pictilisib (dimethanesulfonate)

Item no.	HY-20180-10mM
Manufacturer	MedChem Express
CASRN	957054-33-0
Amount	10mM/1mL
Quantity options	100 mg 10mM/1mL 10 mg 200 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Clone	N/A
Specific against	other
Purity	99.70
Formula	C25H35N7O9S4
Citations	Cell Rep. 2020 Sep 29;32(13):108196.<br/>Biochem J. 2022 Oct 14;479(19):2131-2151.<br/>Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. <br/>bioRxiv. 2020 Mar.<br/>Br J Cancer. 2021 Mar 15.<br/>Cancer Discov. 2012 May;2(5):425-33.<br/>Cancer Res. 2014 Jan 1;74(1):15-23.<br/>Cancer Res. 2024 Jun 17.<br/>Cancers. 2020 Jul 16;12(7):1918.<br/>Cell Biosci. 2022 Aug 21;12(1):135.<br/>Cell Cycle. 2019 Jul;18(13):1513-1522. <br/>Cell Metab. 2012 Mar 7;15(3):382-94.<br/>Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.<br/>Cell Rep. 2023 May 29;42(6):112570.<br/>Cell Syst. 2020 Jan 22;10(1):66-81.e11.<br/>Cell. 2023 Jun 22;186(13):2929-2949.e20.<br/>Debreceni egyettemmolekularis orvostudomany. 2024 Dec.<br/>Harvard Medical School LINCS LIBRARY<br/>Int J Clin Exp Pathol. 2017;10(3):3033-3042.<br/>Int J Oncol. 2017 Sep;51(3):823-831.<br/>J Cell Biol. 2020 Dec 7;219(12):e202001031.<br/>J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246.<br/>J Clin Invest. 2022 Nov 22;e153470.<br/>J Surg Res. 2022 Oct 20;282:137-146.<br/>Molecules. 2019 Apr 1;24(7):1260.<br/>Molecules. 2020 Apr 23;25(8):1980.<br/>Nat Biomed Eng. 2018 Aug;2(8):578-588.<br/>Nat Cancer. 2024 Mar;5(3):433-447.<br/>Nat Chem Biol. 2017 Jan;13(1):38-45.<br/>Nat Commun. 2015 Oct 7;6:8501. <br/>Nat Commun. 2016 Feb 2;7:10438.<br/>Nature. 2018 Aug;560(7719):499-503.<br/>Oncogene. 2016 Jun 9;35(23):2961-70. <br/>Oncol Lett. 2023 Nov 15.<br/>Oncol Rep. 2023 May 9.<br/>Oncotarget. 2016 Aug 16;7(33):53515-53525.<br/>Oncotarget. 2016 May 31;7(22):32641-51. <br/>Patent. US20220313694A1.<br/>Sci Rep. 2021 Jan 11;11(1):291.<br/>Sci Signal. 2021 Dec 21;14(714):eabj0057.<br/>Sci Transl Med. 2013 Jul 31;5(196):196ra99.<br/>Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.<br/>Tierärztliche Hochschule Hannover. 2021 Jul.<br/>Transl Oncol. January 2022, 101260.<br/>[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.<br/>[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.<br/>[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.<br/>[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<br/>[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.
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	GDC-0941 (dimethanesulfonate) ; GDC-0941 (2 MeSO3H salt)
Available
Product 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).
StorageTemperature	4°C (Powder, sealed storage, away from moisture)
Shipping	Room Temperature
Manufacturers Applications	Cancer-Kinase/protease
MolecularWeight	705.85
Clinical Information	Phase 2
Manufacturers Research Area	Cancer
Solubility	DMSO : 7.14 mg/mL (ultrasonic; warming)\|H2O : 7.14 mg/mL (ultrasonic; warming; heat to 60°C)
Target	Apoptosis; Autophagy; PI3K
Manufacturers Target	Apoptosis; Autophagy; PI3K
Isoform	PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
Manufacturers Pathway	Apoptosis; Autophagy; PI3K/Akt/mTOR
Manufacturers Product type	Reference compound

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HY-20180-10mM-safety-datasheet.pdf