BYL-719 (Synonyms: BYL 719; BYL719) |
رقم الكتالوجGC16462
One-Click Copy Product Info
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BYL-719 (BYL-719) هو مثبط فعال وانتقائي وفموي لـ PI3Kα. يظهر BYL-719 (BYL-719) فاعلية في استهداف سرطان PIK3CA المحول. كما يثبط BYL-719 (BYL-719) p110α/p110γ/p110δ/p110β بتراكيز IC50 تبلغ 5/250/290/1200 نانومتر على التوالي. نشاط مضاد للأورام.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1217486-61-7
Sample solution is provided at 25 µL, 10mM.
BYL-719 is an orally available phosphatidylinositol 3-kinase (PI3K) inhibitor that blocks the PI3K/AKT/mTOR pathway[1]. BYL-719 specifically inhibits the activity of PI3K p110α (the catalytic subunit of PI3K), and suppresses block the transformation of PIP2 to PIP3, as well as MAPK/ERK signaling pathways to disrupt the tumor microenvironment[2]. BYL-719 has been widely used to inhibit the proliferation of various drug-resistant breast cancer cells[3].
In vitro, BYL-719 treatment for 96 hours significantly inhibited the viability of MCF-7 and T47D cells, with IC50 values of 0.225μM and 3.055μM, respectively[4]. Treatment with 10μM BYL-719 for 72 hours significantly induced apoptosis in Lip1 cells and reduced the expression of PCNA, GLUT1 and PGK mRNA[5]. Treatment with 5μM BYL-719 for 24 hours reduced the phosphorylation levels of AKT and S6K1 in SNU638 cells and induced G0/G1 phase arrest[6].
In vivo, BYL-719 treatment via oral administration at a dose of 10mg/kg/day for 15 days significantly reduced body weight in obese (ob/ob) mice[7]. Oral administration of BYL-719 at a dose of 0.3g/kg daily for 12 months significantly extended the lifespan and enhanced the strength and balance ability of mice[8].
References:
[1] Markham A. Alpelisib: first global approval[J]. Drugs, 2019, 79(11): 1249-1253.
[2] Kawczak P, Bączek T. Molecular Profiling and Targeted Therapeutic Strategies in Breast Cancer: Clinical Integration of HER2, CDK4/6, and PI3K Inhibition with Trastuzumab, Abemaciclib and Alpelisib[J]. Journal of Clinical Medicine, 2026, 15(10): 3715.
[3] Boyd D C, Zboril E K, Olex A L, et al. Discovering synergistic compounds with BYL-719 in PI3K overactivated basal-like PDXs[J]. Cancers, 2023, 15(5): 1582.
[4] Yu L, Zang C, Ye Y, et al. Effects of BYL-719 (alpelisib) on human breast cancer stem cells to overcome drug resistance in human breast cancer[J]. Frontiers in Pharmacology, 2024, 15: 1443422.
[5] Kirstein A S, Augustin A, Penke M, et al. The novel phosphatidylinositol-3-kinase (PI3K) inhibitor alpelisib effectively inhibits growth of PTEN-haploinsufficient lipoma cells[J]. Cancers, 2019, 11(10): 1586.
[6] Kim K J, Kim J W, Sung J H, et al. PI3K-targeting strategy using alpelisib to enhance the antitumor effect of paclitaxel in human gastric cancer[J]. Scientific reports, 2020, 10(1): 12308.
[7] Lopez-Guadamillas E, Muñoz-Martin M, Martinez S, et al. PI3Kɑ inhibition reduces obesity in mice[J]. Aging (Albany NY), 2016, 8(11): 2747.
[8] Hedges C P, Shetty B, Broome S C, et al. Dietary supplementation of clinically utilized PI3K p110α inhibitor extends the lifespan of male and female mice[J]. Nature Aging, 2023, 3(2): 162-172.
| Cell experiment [1]: | |
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Cell lines |
MCF-7 cells |
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Preparation Method |
MCF-7 cells were cultured in RPMI 1640 medium containing with 10% fetal bovine serum (FBS), and 1% penicillin-streptomycin at 37°C in 5% CO2/atmosphere. MCF-7 cells were seeded onto 96-well microplates (5×103 cells/well) and cultured for 24h. Cells were treated with the different concentrations of BYL-719 (0, 0.01, 0.1, 1, and 10μM) in the presence of 10% FBS for 48h, cell viability was detected. |
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Reaction Conditions |
0, 0.01, 0.1, 1, and 10μM; 48h |
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Applications |
BYL-719 treatment decreased the cell viability of MCF-7 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Ob/ob C57BL6J mice |
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Preparation Method |
Ob/ob C57BL6J mice (20 weeks old) were housed under controlled temperature (21-23°C), humidity (30-35%) and light cycle (8:00 AM to 8:00 PM) and maintained on a standard chow diet with 18% of fat-based caloric content. BYL-719 (10mg/kg) was administered daily by oral gavage for 15 days. Daily record of the mice's weight. |
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Dosage form |
10mg/kg/day; 15 days; p.o. |
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Applications |
BYL-719 treatment significantly reduced body weight in ob/ob mice. |
References: [1] Yu L, Zang C, Ye Y, et al. Effects of BYL-719 (alpelisib) on human breast cancer stem cells to overcome drug resistance in human breast cancer[J]. Frontiers in Pharmacology, 2024, 15: 1443422. [2] Lopez-Guadamillas E, Muñoz-Martin M, Martinez S, et al. PI3Kɑ inhibition reduces obesity in mice[J]. Aging (Albany NY), 2016, 8(11): 2747. | |
| Cas No. | 1217486-61-7 | SDF | |
| المرادفات | BYL 719; BYL719 | ||
| Chemical Name | (2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide | ||
| Canonical SMILES | CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F | ||
| Formula | C19H22F3N5O2S | M.Wt | 441.47 |
| الذوبان | ≥ 22.1mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2652 mL | 11.3258 mL | 22.6516 mL |
| 5 mM | 453 μL | 2.2652 mL | 4.5303 mL |
| 10 mM | 226.5 μL | 1.1326 mL | 2.2652 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)