Structure of Pictilisib
CAS No.: 957054-30-7
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Pictilisib (GDC-0941) is a potent PI3Kα/δ inhibitor with an IC50 of 3 nM, showing modest selectivity against p110β (11-fold) and p110γ (25-fold).
Synonyms: GDC-0941; GNE-0941; Pictrelisib
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CAS No. : | 957054-30-7 |
Formula : | C23H27N7O3S2 |
M.W : | 513.64 |
SMILES Code : | CS(=O)(=O)N1CCN(CC2=CC3=C(S2)C(=NC(=N3)C2=C3C=NNC3=CC=C2)N2CCOCC2)CC1 |
Synonyms : |
GDC-0941; GNE-0941; Pictrelisib
|
MDL No. : | MFCD11616196 |
InChI Key : | LHNIIDJUOCFXAP-UHFFFAOYSA-N |
Pubchem ID : | 17755052 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H332-H335 |
Precautionary Statements: | P280-P305+P351+P338-P310 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
MEB-Med-8A cells | 1 μM | 24 h | Pictilisib significantly inhibited the migration of MEB-Med-8A cells and altered the cytoskeleton structure. | PMC9716228 |
Daoy cells | 1 μM | 24 h | Pictilisib reduced the migration of Daoy cells, significantly decreased wound closure, and altered the cytoskeleton structure. | PMC9716228 |
KPwmC cells | 1μM | 30 min | To observe the effect of Pictilisib on p-CREB1S133 levels, results showed that Pictilisib reduced p-CREB1S133 levels. | PMC8338884 |
P14 CD8+ T cells | 1 μM | 3 to 4 days | Inhibition of PI3K activity, leading to defective CD3 polarity and Glut1 surface trafficking, reduced glucose uptake | PMC5806629 |
SW48-HER2 | 0.05 to 10 μM | 96 h | To evaluate the anti-proliferative effects of Pictilisib on SW48-HER2 cells. Results showed that Pictilisib as a single agent exhibited dose-dependent cell growth inhibition in HER2-amplified cells. | PMC6549349 |
LIM1215-HER2 | 0.05 to 10 μM | 96 h | To evaluate the anti-proliferative effects of Pictilisib on LIM1215-HER2 cells. Results showed that Pictilisib as a single agent exhibited dose-dependent cell growth inhibition in HER2-amplified cells. | PMC6549349 |
SW48-HER2 cells | 0.05 to 10 μM | 96 h | To evaluate the inhibitory effect of Pictilisib on cell proliferation, the results showed that Pictilisib monotherapy exhibited dose-dependent growth inhibition in HER2-amplified cells. | PMC6549349 |
LIM1215-HER2 cells | 0.05 to 10 μM | 96 h | To evaluate the inhibitory effect of Pictilisib on cell proliferation, the results showed that Pictilisib monotherapy exhibited dose-dependent growth inhibition in HER2-amplified cells. | PMC6549349 |
MIMCD3 cells | 1 µM | 10 h | Pictilisib significantly reduced phosphorylation of Akt, MAPKAP1, and GFAP, and increased the formation of Dendra2 CMA reporter puncta, indicating an increase in CMA activity. | PMC7557678 |
AML12 cells | 2 µM | 10 h | Pictilisib significantly reduced phosphorylation of Akt, MAPKAP1, and GFAP, and increased the formation of Dendra2 CMA reporter puncta, indicating an increase in CMA activity. | PMC7557678 |
NIH3T3 cells | 500 nM | 10 h | Pictilisib significantly reduced phosphorylation of Akt, MAPKAP1, and GFAP, and increased the accumulation of Dendra2 CMA reporter puncta, indicating an increase in CMA activity. | PMC7557678 |
Human NK cells | 1 μM | 2 hours | To evaluate the effect of MLN1117 on human NK cell-mediated cytotoxicity. Results showed that selective inhibition of p110α had minimal impact on human NK cell-mediated cytotoxicity. | PMC4051752 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Nude mice | LIM1215-HER2 and SW48-HER2 tumor xenograft models | Oral | 75 mg/kg | Once daily for 4 weeks | To evaluate the antitumor activity of Pictilisib in LIM1215-HER2 and SW48-HER2 tumor xenograft models. Results showed that Pictilisib as a single agent had little effect on tumor growth, but the combination with Refametinib almost completely suppressed tumor growth. | PMC6549349 |
Nude mice | LIM1215-HER2 and SW48-HER2 tumor xenografts | Oral | 75 mg/kg | Every day, for 4 weeks | To evaluate the inhibitory effect of Pictilisib monotherapy and its combination with Refametinib on tumor growth, the results showed that the combination therapy significantly suppressed tumor growth and lasted up to 20 weeks after the end of treatment. | PMC6549349 |
Mice | Normal 3-month-old mice | Oral | 100 mg/kg | Once per day for 7 days | Pictilisib significantly increased CMA substrate uptake in liver lysosomes and reduced lysosomal GFAP phosphorylation in mice, indicating an increase in CMA activity. | PMC7557678 |
Mice | MR86 patient-derived xenograft (PDX) model | Oral | 150 mg/kg | Once daily for up to 40 days | To evaluate the inhibitory effect of Pictilisib in combination with Erdafitinib on tumor growth, the results showed that the combination treatment significantly inhibited tumor growth | PMC10481128 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT02430363 | Glioblastoma | Phase 1 Phase 2 | Unknown | June 2018 | United States, Massachusetts ... More >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 Belgium UCL- Cliniques Universitaires Saint Luc Brussels, Belgium Germany St Johannes Hospital Duisburg, Germany, 47166 Italy Spedali Civili di Brescia Brescia, Italy IRCCS San Raffaele Milan, Italy Poland Lower-Silesian Oncology Centre Wroclaw, Lower-Silesian, Poland, 53413 Russian Federation Pavlov State Medical University St. Petersburg, Russian Federation, 197089 Spain Hospital Universitario Germans Trias I Pujol Barcelona,, Spain Switzerland Universitätsklinik für Frauenheilkunde Bern, Switzerland Ukraine Regional Cancer Center Dnepropetrovsk, Ukraine, 49000 National Institute of Cancer Kiev, Ukraine, 03035 United Kingdom Royal Victoria Hospital Belfast, Ulster, United Kingdom, BT12 6BA Less << |
NCT02389842 | Advanced Solid Tumours ... More >> Breast Cancer Less << | Phase 1 | Unknown | August 2017 | United Kingdom ... More >> The Royal Marsden NHS Foundation Trust Recruiting London, United Kingdom, SM2 5PT Contact: Timothy Yap, PhD 02086613539 timothy.yap@icr.ac.uk Principal Investigator: Timothy Yap, PhD The Christie NHS Foundation Trust Not yet recruiting Manchester, United Kingdom, M20 4BX Contact: Anne Amstrong, MBBS 0161 446 3746 elaine.mercer@christie.nhs.uk Principal Investigator: Anne Armstrong, MBBS Less << |
NCT02092831 | Healthy Volunteer | Phase 1 | Completed | - | United States, Wisconsin ... More >> Madison, Wisconsin, United States, 53704 Less << |
NCT00960960 | Breast Cancer | Phase 1 | Completed | - | United States, Illinois ... More >> Peoria, Illinois, United States, 61615 United States, Massachusetts Boston, Massachusetts, United States, 02115 United States, Tennessee Nashville, Tennessee, United States, 37232 Belgium Leuven, Belgium, 3000 Italy Milano, Lombardia, Italy, 20133 Less << |
NCT00974584 | Non-Squamous Non-Small Cell Lu... More >>ng Cancer Less << | Phase 1 | Completed | - | United States, New York ... More >> Buffalo, New York, United States, 14263 France Villejuif, France, 94805 Netherlands Groningen, Netherlands, 9700 RB Less << |
NCT01493843 | Non-Small Cell Lung Cancer | Phase 2 | Completed | - | - |
NCT00999128 | Healthy Volunteers | Phase 1 | Completed | - | United States, California ... More >> Genentech Trial Information Support South San Francisco, California, United States, 94080 Less << |
NCT01437566 | Breast Cancer | Phase 2 | Completed | - | - |
NCT00996892 | Solid Tumors | Phase 1 | Terminated(A recommended Phase... More >> 2 dose and schedule was not identified and the study was terminated before initiation of Stage 2B.) Less << | - | United States, Maryland ... More >> Baltimore, Maryland, United States, 21231 United States, Massachusetts Boston, Massachusetts, United States, 02114 Boston, Massachusetts, United States, 02215 United States, Michigan Detroit, Michigan, United States, 48201 United States, Oklahoma Oklahoma City, Oklahoma, United States, 73104 United States, Tennessee Nashville, Tennessee, United States, 37203 Less << |
NCT00928330 | Metastatic Breast Cancer | Phase 1 | Completed | - | United States, Indiana ... More >> Indianapolis, Indiana, United States, 46202 United States, Maryland Baltimore, Maryland, United States, 21231 United States, Massachusetts Boston, Massachusetts, United States, 02115 Less << |
NCT01240226 | Healthy Volunteer | Phase 1 | Completed | - | United States, Texas ... More >> Investigational Site Austin, Texas, United States, 78744 Less << |
NCT00975182 | Non-Squamous Non-Small Cell Lu... More >>ng Cancer, Solid Cancers Less << | Phase 1 | Completed | - | United States, Colorado ... More >> Aurora, Colorado, United States, 80045 United States, New Jersey New Brunswick, New Jersey, United States, 08903 Netherlands Amsterdam, Netherlands, 1066 EC Utrecht, Netherlands, 3508 GA Less << |
NCT01474668 | Healthy Volunteer | PHASE1 | COMPLETED | 2025-10-11 | Madison, Wisconsin, 53704-2523... More >>, United States Less << |
NCT00996892 | - | Terminated(A recommended Phase... More >> 2 dose and schedule was not identified and the study was terminated before initiation of Stage 2B.) Less << | - | - | |
NCT00876122 | Non-Hodgkin's Lymphoma, Solid ... More >>Cancers Less << | PHASE1 | COMPLETED | 2025-07-12 | Sutton, SM2 5PT, United Kingdo... More >>m Less << |
NCT01918306 | Estrogen Receptor Negative Bre... More >>ast Cancer Human Epidermal Growth Factor 2 Negative Carcinoma of Breast Triple Negative Breast Cancer Recurrent Breast Cancer Stage IV Breast Cancer Triple-negative Breast Cancer Less << | Phase 1 Phase 2 | Terminated(company stopped pro... More >>duction of study drug due to excessive toxicities, lack of efficacy) Less << | - | United States, Alabama ... More >> University of Alabama Birmingham, Alabama, United States United States, California University of California, San Francisco San Francisco, California, United States United States, District of Columbia Georgetown University Washington, D.C., District of Columbia, United States United States, Georgia Emory University Atlanta, Georgia, United States United States, Illinois University of Chicago Chicago, Illinois, United States United States, Indiana Indiana University Indianapolis, Indiana, United States United States, Maryland John Hopkins University Baltimore, Maryland, United States United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States United States, Michigan University of Michigan Ann Arbor, Michigan, United States United States, Minnesota Mayo Clinic Rochester, Minnesota, United States United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States United States, North Carolina University of North Carolina Charlotte, North Carolina, United States United States, Pennsylvania University of Pittsburgh Pittsburgh, Pennsylvania, United States United States, Tennessee Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 United States, Texas Baylor Breast Center Houston, Texas, United States United States, Washington University of Washington Seattle, Washington, United States Less << |
NCT01740336 | Breast Cancer | Phase 2 | Completed | - | - |
NCT01918306 | - | Terminated(company stopped pro... More >>duction of study drug due to excessive toxicities, lack of efficacy) Less << | - | - | |
NCT00876109 | Solid Cancers | PHASE1 | COMPLETED | 2025-11-13 | Scottsdale, Arizona, 85258, Un... More >>ited States|Boston, Massachusetts, 02215, United States|Detroit, Michigan, 48201, United States Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.19mL |
9.73mL 1.95mL 0.97mL |
19.47mL 3.89mL 1.95mL |
Tags: Pictilisib | GDC-0941 | GDC0941 | GDC 0941 | PI3K | Autophagy | Apoptosis | Phosphoinositide 3-kinase | inhibit | PI3K inhibitor | cell cycle arrest | NSCLC | PI3Kα | PI3Kδ | 957054-30-7
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