Pictilisib dimethanesulfonate
Based on 68 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- Purity: 99.72%
- CAS No.: 957054-33-0
- Formula: C25H35N7O9S4
- Molecular Weight:705.85
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Pictilisib dimethanesulfonate
More- Nature. 2018 Aug;560(7719):499-503. [Abstract]
- Cell. 2025 May 29;188(11):3065-3080.e21. [Abstract]
- Cell. 2023 Jun 22;186(13):2929-2949.e20. [Abstract]
- Cell Metab. 2021 Nov 2;33(11):2247-2259.e6. [Abstract]
- Cell Metab. 2012 Mar 7;15(3):382-94. [Abstract]
- Gastroenterology. 2025 Oct 27:S0016-5085(25)05903-7. [Abstract]
- Cancer Discov. 2012 May;2(5):425-33. [Abstract]
- Nat Cancer. 2024 Mar;5(3):433-447. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Cancer Res. 2024 Sep 16;84(18):2985-3003. [Abstract]
- Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2016 Feb 2:7:10438. [Abstract]
- Nat Commun. 2015 Oct 7:6:8501. [Abstract]
- Mol Cell. 2025 Aug 7;85(15):2973-2987.e6. [Abstract]
- Nat Chem Biol. 2025 Mar;21(3):432-442. [Abstract]
- Nat Chem Biol. 2017 Jan;13(1):38-45. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]
- J Clin Invest. 2023 Jan 17;133(2):e153470. [Abstract]
- Adv Sci (Weinh). 2026 Mar;13(13):e01810. [Abstract]
- MedComm (2020). 2024 Aug 12;5(8):e684. [Abstract]
- J Pharm Anal. 2025 May;15(5):101092. [Abstract]
- Cell Death Discov. 2026 Feb 25;12(1):111. [Abstract]
- Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]
- Free Radic Biol Med. 2025 Oct 30:242:275-287. [Abstract]
- Br J Cancer. 2021 Apr;124(9):1581-1591. [Abstract]
- Cell Rep. 2023 May 29;42(6):112570. [Abstract]
- Cell Rep. 2020 Sep 29;32(13):108196. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Int J Oncol. 2017 Sep;51(3):823-831. [Abstract]
- Sci Signal. 2025 Sep 2;18(902):eadw3231. [Abstract]
- Sci Signal. 2021 Dec 21;14(714):eabj0057. [Abstract]
- Lipids Health Dis. 2024 Sep 4;23(1):282. [Abstract]
- Cell Biosci. 2022 Aug 21;12(1):135. [Abstract]
- J Cell Biol. 2020 Dec 7;219(12):e202001031. [Abstract]
- J Clin Endocrinol Metab. 2021 Jan 1;106(1):e232-e246. [Abstract]
- Bioorg Chem. 2026 Jun 5:173:109635. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- Molecules. 2019 Apr 1;24(7):1260. [Abstract]
- Transl Oncol. 2022 Jan;15(1):101260. [Abstract]
- Sci Rep. 2021 Jan 11;11(1):291. [Abstract]
- Cancers (Basel). 2020 Jul 16;12(7):1918. [Abstract]
- Oncol Rep. 2023 Jul;50(1):131. [Abstract]
- J Virol. 2025 Aug 25:e0022125. [Abstract]
- Biochem J. 2022 Oct 14;479(19):2131-2151. [Abstract]
- Cell Cycle. 2019 Jul;18(13):1513-1522. [Abstract]
- Cancer Med. 2025 Sep;14(18):e71227. [Abstract]
- Chem Biodivers. 2025 Apr;22(4):e202403291. [Abstract]
- Biochem Biophys Res Commun. 2025 Aug 30:776:152203. [Abstract]
- Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. [Abstract]
- Oncol Lett. 2023 Nov 15;27(1):18. [Abstract]
- Anticancer Res. 2025 Apr;45(4):1355-1366. [Abstract]
- J Surg Res. 2023 Feb:282:137-146. [Abstract]
- Arab J Gastroenterol. 2025 Feb;26(1):104-111. [Abstract]
- Int J Clin Exp Pathol. 2017;10(3):3033-3042.
- bioRxiv. 2026 Mar 25.
- bioRxiv. 2026 Feb 17:2026.02.14.705941. [Abstract]
- bioRxiv. 2025 Sep 20:2025.09.17.676669. [Abstract]
- bioRxiv. 2025 Jul 23:2025.07.18.665614. [Abstract]
- Research Square Preprint. 2024 Nov 26.
- Patent. US20210236501A1.
- Debreceni egyettemmolekularis orvostudomany. 2024 Dec.
- Patent. US20220313694A1.
- Tierärztliche Hochschule Hannover. 2021 Jul.
- bioRxiv. 2020 Mar.
- Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]
- Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]
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Cell Proliferation/Viability Assay
Biological Activity
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p110α 3 nM (IC50) |
p110α-H1047R 3 nM (IC50) |
p110α-E545K 3 nM (IC50) |
p110δ 3 nM (IC50) |
p110β 33 nM (IC50) |
p110γ 75 nM (IC50) |
mTOR 0.58 μM (Ki) |
DNA-PK 1.23 μM (IC50) |
Autophagy |
Pictilisib (GDC-0941) and RP-56976 reduce tumor cell viability by 80% or greater in the breast cancer cell lines than single-agent treatment. GDC-0941 inhibits Akt phosphorylation and downstream targets of Akt signaling such as pPRAS40 and pS6 in Hs578T1.2 (PI3Kα wild-type), MCF7-neo/HER2 (PI3Kα-mutant), and MX-1 (PTEN-null) tumor models. Pictilisib (GDC-0941) decreases the time of RP-56976-induced mitotic arrest prior to apoptosis[1]. Pictilisib (GDC-0941) shows a high efficacy of antitumor activity in two ZD1839-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460. Pictilisib (GDC-0941) is highly efficacious in combination with U0126 in inducing cell growth inhibition, G0-G1 arrest and cell apoptosis. H460 cells with activating mutations of PIK3CA are relatively more sensitive to Pictilisib (GDC-0941) than A549 cells with wild-type PIK3CA[3]. Pictilisib (GDC-0941) reduces PI3K pathway activity in both cell lines, illustrated by decreased pAK. Pictilisib (GDC-0941) significantly reduces secreted VEGF detected in the medium after hypoxic/anoxic exposure in all cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 957054-33-0
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Appearance Solid
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Molecular Weight 705.85
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Formula C25H35N7O9S4
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Color White to light yellow
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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
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Synonyms
GDC-0941 dimethanesulfonate ; GDC-0941 (2 MeSO3H salt)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (68)
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Journal Impact Factor
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Most Recent
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Nature
2018 Aug;560(7719):499-503. PMID: 30051890 -
Cell
Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]2025 May 29;188(11):3065-3080.e21. PMID: 40393457 -
Cell
Distinct longevity mechanisms across and within species and their association with aging. [Abstract]2023 Jun 22;186(13):2929-2949.e20. PMID: 37269831 -
Cell Metab
2021 Nov 2;33(11):2247-2259.e6. PMID: 34731655 -
Cell Metab
2012 Mar 7;15(3):382-94. PMID: 22405073
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2012 Mar 7;15(3):382-94. [Abstract]
Effect of the indicated PI3K inhibitors on pre-brown adipocytes. Cultures are treated with the inhibitors at the indicated concentrations (μM) for 4 h. Protein levels (top) and mRNA levels (bottom) of the indicated proteins and genes, respectively, are analyzed. Assays are performed in triplicate cultures. Values represent mean ± sd, and statistical significance is determined by the two-tailed Student’s t-test. *p<0.05, **p<0.01.
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Gastroenterology
Targeting Mutual Dependence of Phosphatidylinositol-3-Kinase α/δ and Small Ubiquitin-Like Modifier Signaling in Pancreatic Cancer. [Abstract]2025 Oct 27:S0016-5085(25)05903-7. PMID: 41143762 -
Cancer Discov
Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. [Abstract]2012 May;2(5):425-33. PMID: 22588880
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2012 May;2(5):425-33. [Abstract]
Effects of KIN-193, GDC-0941, PIK-75 and IC87114 on AKT phosphorylation in PTEN-deficient cell lines as indicated. Representative western blots are shown. Bar graphs represent mean ± SD of western blot quantitations of AKTT308 (n=3).
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Nat Cancer
Loss of Pip4k2c confers liver-metastatic organotropism through insulin-dependent PI3K-AKT pathway activation. [Abstract]2024 Mar;5(3):433-447. PMID: 38286827 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Cancer Res
Oncogenic Calreticulin Induces Immune Escape by Stimulating TGF-β Expression and Regulatory T Cell Expansion in the Bone Marrow Microenvironment. [Abstract]2024 Sep 16;84(18):2985-3003. PMID: 38885318 -
Cancer Res
A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. [Abstract]2014 Jan 1;74(1):15-23. PMID: 24322983 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
Stabilization of p21 by mTORC1/4E-BP1 predicts clinical outcome of head and neck cancers. [Abstract]2016 Feb 2:7:10438. PMID: 26832959
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2016 Feb 2:7:10438. [Abstract]
Western blot illustrating the effect of PI3K inhibitors on p21 protein levels in MEFs. Cells are treated for 24 hours with the indicated concentrations of the different drugs.
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Nat Commun
A PI3K p110β-Rac signalling loop mediates Pten-loss-induced perturbation of haematopoiesis and leukaemogenesis. [Abstract]2015 Oct 7:6:8501. PMID: 26442967 -
Mol Cell
2025 Aug 7;85(15):2973-2987.e6. PMID: 40712585 -
Nat Chem Biol
2025 Mar;21(3):432-442. PMID: 39482470 -
Nat Chem Biol
2017 Jan;13(1):38-45. PMID: 27820799 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Transl Med
mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. [Abstract]2013 Jul 31;5(196):196ra99. PMID: 23903756
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]
Sensitivity to GDC-0941 in parental MDA453 and T47D and BYL719-resistant MDA453R and T47DR cells. Protein lysates are isolated after 24 hours of treatment with 1 μM GDC-0941 and probed against the indicated proteins.
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J Clin Invest
Oncogenic KRAS signaling drives evasion of innate immune surveillance in lung adenocarcinoma by activating CD47. [Abstract]2023 Jan 17;133(2):e153470. PMID: 36413402 -
Adv Sci (Weinh)
IL1R2 Marks and Sorts a Spermatogonial Stem Cell Population Critical for Restoring Spermatogenesis Upon Interruption in Mammals. [Abstract]2026 Mar;13(13):e01810. PMID: 41486830 -
MedComm (2020)
Ubiquitin-specific protease 22 controls melanoma metastasis and vulnerability to ferroptosis through targeting SIRT1/PTEN/PI3K signaling. [Abstract]2024 Aug 12;5(8):e684. PMID: 39135915 -
J Pharm Anal
Screen of FDA-approved drug library identifies vitamin K as anti-ferroptotic drug for osteoarthritis therapy through Gas6. [Abstract]2025 May;15(5):101092. PMID: 40496065 -
Cell Death Discov
The protective up-regulation of metallothionein-2A in intervertebral disc degeneration inhibits nucleus pulposus cell ferroptosis through activation of the PI3K/AKT/mTOR pathway. [Abstract]2026 Feb 25;12(1):111. PMID: 41741409 -
Oncogene
PIK3CA(H1047R)- and Her2-initiated mammary tumors escape PI3K dependency by compensatory activation of MEK-ERK signaling. [Abstract]2016 Jun 9;35(23):2961-70. PMID: 26640141
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]
Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC+PIK3CAH1047R tumors treated as indicated.
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Free Radic Biol Med
7,8-Dihydroxyflavone protects acetaminophen induced liver injury through activating PI3K/Akt/NRF2/GPX4 mediated ferroptosis suppression. [Abstract]2025 Oct 30:242:275-287. PMID: 41173313 -
Br J Cancer
2021 Apr;124(9):1581-1591. PMID: 33723394 -
Cell Rep
Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]2023 May 29;42(6):112570. PMID: 37252843 -
Cell Rep
2020 Sep 29;32(13):108196. PMID: 32997991 -
Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693 -
Int J Oncol
Downregulation of BRD4 inhibits gallbladder cancer proliferation and metastasis and induces apoptosis via PI3K/AKT pathway. [Abstract]2017 Sep;51(3):823-831. PMID: 28766687
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Sep;51(3):823-831. [Abstract]
Protein levels of BRD4, p-AKT and AKT in GDC-0941 treated NOZ cells after 72 h.
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Sci Signal
MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells. [Abstract]2025 Sep 2;18(902):eadw3231. PMID: 40892895 -
Sci Signal
Suppression of caspase 8 activity by a coronin 1-PI3Kδ pathway promotes T cell survival independently of TCR and IL-7 signaling. [Abstract]2021 Dec 21;14(714):eabj0057. PMID: 34932374 -
Lipids Health Dis
MG-132 activates sodium palmitate-induced autophagy in human vascular smooth muscle cells and inhibits senescence via the PI3K/AKT/mTOR axis. [Abstract]2024 Sep 4;23(1):282. PMID: 39232759 -
Cell Biosci
Anti-tumor effects of dual PI3K-HDAC inhibitor CUDC-907 on activation of ROS-IRE1α-JNK-mediated cytotoxic autophagy in esophageal cancer. [Abstract]2022 Aug 21;12(1):135. PMID: 35989326 -
J Cell Biol
2020 Dec 7;219(12):e202001031. PMID: 33048163 -
J Clin Endocrinol Metab
2021 Jan 1;106(1):e232-e246. PMID: 33000123 -
Bioorg Chem
Eupalinolide B prevents cerebral ischemia-reperfusion injury via the PI3K/Akt/GSK3β(Ser9) signaling pathway. [Abstract]2026 Jun 5:173:109635. PMID: 41719922 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
Molecules
Screening of PI3K-Akt-targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. [Abstract]2019 Apr 1;24(7):1260. PMID: 30939726 -
Transl Oncol
A novel strategy for combination of clofarabine and pictilisib is synergistic in gastric cancer. [Abstract]2022 Jan;15(1):101260. PMID: 34735897 -
Sci Rep
2021 Jan 11;11(1):291. PMID: 33431926 -
Cancers (Basel)
Expression of MALAT1 Promotes Trastuzumab Resistance in HER2 Overexpressing Breast Cancers. [Abstract]2020 Jul 16;12(7):1918. PMID: 32708561 -
Oncol Rep
Aprepitant inhibits the progression of esophageal squamous cancer by blocking the truncated neurokinin‑1 receptor. [Abstract]2023 Jul;50(1):131. PMID: 37203393 -
J Virol
SFTSV utilizes AXL/GAS6 for entry via PI3K-PLC-dependent macropinocytosis activated by AXL-kinase. [Abstract]2025 Aug 25:e0022125. PMID: 40853130 -
Biochem J
Up-regulation of the PI3K/AKT and RHO/RAC/PAK signalling pathways in CHK1 inhibitor resistant Eµ-Myc lymphoma cells. [Abstract]2022 Oct 14;479(19):2131-2151. PMID: 36240067 -
Cell Cycle
HER2-L755S mutation induces hyperactive MAPK and PI3K-mTOR signaling, leading to resistance to HER2 tyrosine kinase inhibitor treatment. [Abstract]2019 Jul;18(13):1513-1522. PMID: 31135266 -
Cancer Med
Focal Adhesion Kinase Intersects With the BRD4-MYC Axis and YAP1 to Drive Tumor Cell Growth, Phenotypic Plasticity, Stemness, and Metastatic Potential in Colorectal Cancer. [Abstract]2025 Sep;14(18):e71227. PMID: 40959971 -
Chem Biodivers
Shikonin Derivative Suppresses Colorectal Cancer Cells Growth via Reactive Oxygen Species-Mediated Mitochondrial Apoptosis and PI3K/AKT Pathway. [Abstract]2025 Apr;22(4):e202403291. PMID: 40022742 -
Biochem Biophys Res Commun
Loss of DNA replication fork protection by TIMELESS degradation supports oncogene-induced senescence. [Abstract]2025 Aug 30:776:152203. PMID: 40517672 -
Bioorg Med Chem Lett
2012 Mar 1;22(5):1874-8. PMID: 22325943 -
Oncol Lett
AKR1B10 inhibits the proliferation and metastasis of hepatocellular carcinoma cells by regulating the PI3K/AKT pathway. [Abstract]2023 Nov 15;27(1):18. PMID: 38034486 -
Anticancer Res
Akt Regulates Extracellular Vesicle Secretion in Hypoxia-adapted Multiple Myeloma RPMI8226 Cells. [Abstract]2025 Apr;45(4):1355-1366. PMID: 40155008 -
J Surg Res
2023 Feb:282:137-146. PMID: 36274448 -
Arab J Gastroenterol
NNMT suppresses H3K9me3 to facilitate malignant progression and drug resistance in gastric cancer. [Abstract]2025 Feb;26(1):104-111. PMID: 39757078 -
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bioRxiv
2026 Feb 17:2026.02.14.705941. PMID: 41756935 -
bioRxiv
Loss of the tumor suppressor PTEN activates cell-intrinsic interferon signaling to drive immune resistance. [Abstract]2025 Sep 20:2025.09.17.676669. PMID: 41000885 -
bioRxiv
Endocrine therapy induces oxidative stress in ER+ breast cancer that sensitizes persister cells to ferroptosis. [Abstract]2025 Jul 23:2025.07.18.665614. PMID: 40777469 -
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Oncotarget
Simultaneous inhibition of Vps34 kinase would enhance PI3Kδ inhibitor cytotoxicity in the B-cell malignancies. [Abstract]2016 Aug 16;7(33):53515-53525. PMID: 27447747
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]
PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.
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Oncotarget
Characterization of selective and potent PI3Kδ inhibitor (PI3KDIN- 015) for B-Cell malignances. [Abstract]2016 May 31;7(22):32641-51. PMID: 27081697
Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]
The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC50 of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.
Solvent & Solubility
H2O : 7.14 mg/mL (10.12 mM; ultrasonic and warming and heat to 60°C)
DMSO : 7.14 mg/mL (10.12 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Cells are treated at EC50 concentrations of Pictilisib (GDC-0941), RP-56976, or both for 4 or 24 hours and lysed in 1×Cell Extraction Buffer supplemented with protease inhibitors and Phosphatase Inhibitor Cocktails 1 and 2. Protein concentrations are determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal amounts of protein are separated by electrophoresis through NuPAGE Bis-Tris 10% gradient gels, transferred onto polyvinylidene difluoride membranes using the Criterion system, and probed with monospecific primary antibodies. Specific antigen-antibody interactions are detected with IRDye 680 or IRDye 800 infrared secondary antibodies using a LI-COR imaging system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female nu/nu mice are inoculated subcutaneously with MCF7-neo/HER2 or MX-1 breast cancer cells. When tumors reach a mean volume of 200 to 250 mm3, animals are size-matched and distributed into groups consisting of 10 animals per group. RP-56976 formulated in 3% EtOH, 97% saline is administered intravenously once weekly. Pictilisib (GDC-0941), formulated in MCT (0.5% methylcellulose, 0.2% Tween-80) is dosed orally and daily. MAXF1162 is an HER2+/ER+/PR+ patient-derived breast cancer tumor xenograft model established by directly implanting tumors subcutaneously from patient to NMRI nu/nu mice. Tumor volume is calculated. Tumor sizes are recorded twice weekly over the course of a study.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[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. [Content Brief]
[5]. 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 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.4167 mL | 7.0837 mL | 14.1673 mL | 35.4183 mL |
| 5 mM | 0.2833 mL | 1.4167 mL | 2.8335 mL | 7.0837 mL | |
| 10 mM | 0.1417 mL | 0.7084 mL | 1.4167 mL | 3.5418 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.