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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H22F3N3O3 |
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分子量 | 433.42 | CAS No. | 1372540-25-4 | |
Solubility (25°C)* | 体外 | DMSO | 86 mg/mL (198.42 mM) | |
Ethanol | 1 mg/mL (2.3 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines. |
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in vitro | GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. [1] GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. [2] |
in vivo | GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice. [1] |
細胞アッセイ | 細胞株 | p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines. |
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濃度 | ~10 μM | |
反応時間 | 72 hours | |
実験の流れ | Cells are plated in 96-well microtiter plates at densities ranging from 1,500 to 15,000 cells/well, optimized for untreated control cells to be 80-90% confluent at the endpoint of the experiment. After 24 h, cells are treated with serial dilutions (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). At least three independent experiments in triplicate per cell line targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test (GraphPad Prism), and a two-tailed P value <0.05 is considered statistically significant. |
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動物実験 | 動物モデル | Balb-c nude mice |
投薬量 | 100 mg/kg | |
投与方法 | oral administration |
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, , Clin Cancer Res, 2017, 23(11):2795-2805
, , Dr. Antonino Maria Spartà from University of Bolog
Data from [Data independently produced by , , FASEB J, 2018, doi:10.1096/fj.201800183R]
Idelalisib activates AKT via increased recruitment of PI3Kδ/PI3Kβ to BCR signalosome while reducing PDK1 in post-therapy CLL cells [ Leukemia, 2022, 10.1038/s41375-022-01595-0] | PubMed: 35568768 |
PI3K Isoform-Specific Regulation of Leader and Follower Cell Function for Collective Migration and Proliferation in Response to Injury [ Cells, 2022, 11(21)3515] | PubMed: 36359913 |
Computational analysis of cholangiocarcinoma phosphoproteomes identifies patient-specific drug targets [ Cancer Res, 2021, canres.0955.2021] | PubMed: 34551960 |
Cisplatin Resistance in Osteosarcoma: In vitro Validation of Candidate DNA Repair-Related Therapeutic Targets and Drugs for Tailored Treatments. [ Front Oncol, 2020, 10;10:331] | PubMed: 32211337 |
Targeting effector pathways in RAC1P29S-driven malignant melanoma. [ Small GTPases, 2020, 10.1080/21541248] | PubMed: 32043900 |
Tumor Suppressor miRNA-204-5p Regulates Growth, Metastasis, and Immune Microenvironment Remodeling in Breast Cancer. [ Cancer Res, 2019, 79(7):1520-1534] | PubMed: 30737233 |
Amphiregulin potentiates airway inflammation and mucus hypersecretion induced by urban particulate matter via the EGFR-PI3Kα-AKT/ERK pathway [Wang J, et al. Cell Signal, 2019, 53:122-131] | PubMed: 30291869 |
Prostate-specific membrane antigen cleavage of vitamin B9 stimulates oncogenic signaling through metabotropic glutamate receptors. [ J Exp Med, 2018, 215(1):159-175] | PubMed: 29141866 |
PI3Ka-Akt1-mediated Prdm4 induction in adipose tissue increases energy expenditure, inhibits weight gain, and improves insulin resistance in diet-induced obese mice [ Cell Death Dis, 2018, 9(9):876] | PubMed: 30158592 |
Frequent PTEN loss and differential HER2/PI3K signaling pathway alterations in salivary duct carcinoma: Implications for targeted therapy [Saintigny P, et al. Cancer, 2018, 124(18):3693-3705] | PubMed: 30289966 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。