GDC-0941, a selective and potent PI3K inhibitor, is highly efficacious both in combination with trastuzumab and in the treatment of trastuzumab-resistant cells and tumors. GDC-0941 inhibited the growth of >70% of breast cancer cell lines tested, with EC50's <1 µM. GDC-0941 also demonstrated antitumor activity in preclinical models of breast cancer.
J Nucl Med. 2018 Nov 21.
MEK inhibition induces therapeutic iodine uptake in a murine model of anaplastic thyroid cancer.
GDC-0941 (Pictilisib) purchased from AbMole
ChemMedChem. 2018 Dec 6.
Identifying Lysophosphatidic Acid Acyltransferase β (LPAAT-β) as the Target of a Nanomolar Angiogenesis Inhibitor from a Phenotypic Screen Using the Polypharmacology Browser PPB2.
GDC-0941 (Pictilisib) purchased from AbMole
Mol Cancer Res. 2018 Aug 14.
Comprehensive Genomic Profiling of Patient-matched Head and Neck Cancer Cells: A Preclinical Pipeline for Metastatic and Recurrent Disease.
GDC-0941 (Pictilisib) purchased from AbMole
J Exp Clin Cancer Res. 2018 Sep 21;37(1):234.
The LAT1 inhibitor JPH203 reduces growth of thyroid carcinoma in a fully immunocompetent mouse model.
GDC-0941 (Pictilisib) purchased from AbMole
BioRxiv. 2017 July 18;1-45.
PIK3CAH1047R-induced paradoxical ERK activation results in resistance to BRAFV600E specific inhibitors in BRAFV600E PIK3CAH1047R double mutant thyroid tumors.
GDC-0941 (Pictilisib) purchased from AbMole
Mol Cancer. 2017 May 22;16(1):93.
PIK3CA hotspot mutations differentially impact responses to MET targeting in MET-driven and non-driven preclinical cancer models
GDC-0941 (Pictilisib) purchased from AbMole
Oncotarget. 2017 Apr 11;8(15): 24604–24620.
Combined MEK and Pi3’-kinase inhibition reveals synergy in targeting thyroid cancer in vitro and in vivo
GDC-0941 (Pictilisib) purchased from AbMole
Cell Experiment | |
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Cell lines | U87MG cell line |
Preparation method | Proliferation Assay. The human tumor cell lines used wereobtained from the ATCC. Cells were plated at 4 × 104 cells/ mL and cultured at 37 °C with 5% CO2 in DMEM supplemented with 10% fetal calf serum, and L-glutamine. Test compound was added to replicate wells in a volume of 10 µL such that the final DMSO concentration did not exceed 0.2%. After 4 days of incubation, 10 µL of Alamar Blue reagent was added and developed for 6 h at 37 °C before measuring the fluorescence excitation/emission (wavelength 540/595 nm) using a Victor plate reader. The reported IC50 values are means of at least two independent experiments with variations of less than 20%. |
Concentrations | 0~10µM |
Incubation time | 4 days |
Animal Experiment | |
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Animal models | Human tumor xenografts of U87MG glioblastoma of female NCr athymic mice |
Formulation | 10% DMSO, 5% Tween 20, 85% water |
Dosages | 75 mg/kg once daily |
Administration | oral gavage |
Molecular Weight | 513.64 |
Formula | C23H27N7O3S2 |
CAS Number | 957054-30-7 |
Solubility (25°C) | DMSO 40 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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