Alpelisib GMP is Alpelisib (HY-15244) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 1217486-61-7
- 화학식: C19H22F3N5O2S
- 분자량:441.47
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
IC50: 5 nM (p110α), 250 nM (p110γ), 290 nM (p110δ), 1200 nM (p110β)[1]
Alpelisib GMP (0-5 μM; 14 d) significantly inhibits the clonal growth of MCF-7 and T47D breast cancer cells in 2D colony formation assays[1].
Alpelisib GMP (5 μM; 5 d) reduces the mammosphere formation efficiency of MCF-7 and T47D breast cancer stem cell-like (BCSC-like) cells in a dose-dependent manner[1].
Alpelisib GMP (0-10 μM; 10 d) significantly reduces the spheroid diameter of MCF-7 and T47D breast cancer stem cell-like (BCSC-like) cells in 3D culture systems, and inhibits their stem cell properties and drug resistance[1].
Alpelisib GMP (1 μM; 24 h) significantly reduces the protein levels of the stem cell markers Nanog, Sox2, and OCT3/4 in MCF-7 and T47D breast cancer stem-like cells (BCSC-like cells)[1].
Alpelisib (10 μM; 10 d) inhibits adipogenesis, thereby attenuating adipocyte differentiation of primary LipPD1 lipoma cells in 2D culture systems and reducing the volume of 3D LipPD1 lipospheres[2].
Combination treatment with Alpelisib GMP (10 μM; 4 d) and a 1 μM SGK3 inhibitor (VPS34-IN1 (HY-12795) or SGK3-IN) produces enhanced antiproliferative activity in Alpelisib GMP-resistant MCF7R and T47DR breast cancer cells, with a synergistic effect observed for the Alpelisib+SGK3-IN combination[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human MCF-7 breast cancer monolayer cells, MCF-7 breast cancer stem cell (BCSC)-enriched mammosphere cells, human T47D breast cancer monolayer cells, T47D BCSC-enriched mammosphere cells
-
Concentration:Serial dilutions
-
Incubation Time:96 h
-
Result:Inhibited cell viability in a dose-dependent manner.
Achieved an IC50 of 0.225 μM in MCF-7 monolayer cells.
Achieved an IC50 of 0.453 μM in MCF-7 BCSC-enriched mammosphere cells.
Achieved an IC50 of 3.055 μM in T47D monolayer cells.
Achieved an IC50 of 5.105 μM in T47D BCSC-enriched mammosphere cells.
-
Cell Line:LipPD1, LipPD2, LipPD3 primary lipoma cells
-
Concentration:1-100 µM
-
Incubation Time:24-144 h
-
Result:Attenuated growth of all three lipoma cell cultures alone and in combination with rapamycin.
Maintained stable cell count for 6 days in LipPD1 cells treated with 100 µM.
Exhibited IC50 values for 72 h Hoechst assays of 15.91 µM (LipPD1), 10.06 µM (LipPD2), and 15.79 µM (LipPD3).
Reduced the fraction of Ki-67 positive LipPD1 cells in a concentration-dependent manner: to 0.75 fold (1 µM, p=0.074), 0.55 fold (10 µM, p=0.018), and 0.22 fold (100 µM, p=0.017).
-
Cell Line:LipPD1, LipPD2, LipPD3, Lip3, Lip4 primary lipoma cells
-
Concentration:50 µM
-
Incubation Time:24, 72 h
-
Result:Observed no cell death after 72 h 50 µM treatment in LipPD1 and Lip3 cells.
Detected a slight reduction in viable cells in Lip4 cells.
Detected no additional LDH release in LipPD1, LipPD2, or LipPD3 cells after 24 h or 72 h 50 µM treatment, indicating no induction of cell death.
-
Cell Line:LipPD1 primary lipoma cells
-
Concentration:10-100 µM
-
Incubation Time:24, 48 h
-
Result:Reduced AKT activation (phospho-Thr 308) in 50 µM treated cells.
Reduced mTOR activation (phospho-Ser 2448) in 10 µM and 50 µM treated cells.
Significantly reduced phosphorylation of S6 (phospho-Ser 235/236) for all tested concentrations.
Reduced the fraction of pS6 positive LipPD1 cells to 0.57 fold (10 µM) and 0.01 fold (100 µM).
-
Cell Line:LipPD1 primary lipoma cells
-
Concentration:10 µM
-
Incubation Time:10 days
-
Result:Reduced lipid accumulation in 2D culture, with the fraction of adipocytes decreasing from 54.8% to 29.9%.
Downregulated mRNA expression of differentiation markers: PPARγ to 0.55 fold, adiponectin to 0.54 fold, aP2 to 0.54 fold, and FASN to 0.58 fold.
Reduced 3D spheroid size to 0.78 fold after 4 days and 0.79 fold after 10 days, with significant differences from day 4 onward, while control spheroid size increased to 1.25 fold after 10 days.
Alpelisib GMP (50 mg/kg; i.p.; daily) exerts partial antitumor activity against alpelisib-resistant T47DR breast cancer xenografts, with maximum efficacy achieved when combined with SGK3 knockdown[3].
Alpelisib GMP (25 mg/kg; p.o.; daily; 4 weeks) significantly inhibits tumor growth, reduces tumor cell proliferation, and increases tumor cell apoptosis in a PIK3CA-mutant gastric cancer xenograft model with 100% survival of treated mice over 4 weeks[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (6-week-old female)[3]
-
Dosage:50 mg/kg
-
Administration:i.p.; daily
-
Result:Exerted partial inhibition of MCF7R xenograft tumor growth.
Achieved maximum tumor growth inhibition when combined with SGK3 knockdown, with significantly reduced final tumor volumes and weights compared to vehicle control or SGK3 knockdown alone.\nExerted partial inhibition of T47DR xenograft tumor growth.
Achieved maximum tumor growth inhibition when combined with SGK3 knockdown, with significantly reduced final tumor volumes and weights compared to vehicle control or SGK3 knockdown alone.
-
Animal Model:Balb/c athymic nude mice (female, 5 weeks old, 26-28 g, subcutaneous xenograft of luciferase-expressing PIK3CA-mutant MKN1 human gastric cancer cells)[4]
-
Dosage:25 mg/kg
-
Administration:p.o.; daily; 4 weeks
-
Result:Significantly retarded tumor growth compared to the control group.
Decreased Ki-67 expression (proliferation marker).
Increased TUNEL expression (apoptosis marker).
Maintained stable body weight over the 4-week period.
Achieved 100% survival of treated mice over the 4-week period.
Chemical Information
-
CAS No. 1217486-61-7
-
분자량 441.47
-
화학식 C19H22F3N5O2S
-
SMILES
CC(N=C(S1)NC(N2CCC[C@H]2C(N)=O)=O)=C1C3=CC(C(C)(C(F)(F)F)C)=NC=C3
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Yu L, et al. Effects of BYL-719 (alpelisib) on human breast cancer stem cells to overcome drug resistance in human breast cancer. Front Pharmacol. 2024;15:1443422. Published 2024 Oct 14. [Content Brief]
[2]. Kirstein AS, et al. The Novel Phosphatidylinositol-3-Kinase (PI3K) Inhibitor Alpelisib Effectively Inhibits Growth of PTEN-Haploinsufficient Lipoma Cells. Cancers (Basel). 2019;11(10):1586. Published 2019 Oct 17. [Content Brief]
[3]. Kang T, et al. The SGK3/GSK3β/β-catenin signaling promotes breast cancer stemness and confers resistance to alpelisib therapy. Int J Biol Sci. 2025;21(6):2462-2475. Published 2025 Mar 19. [Content Brief]
[4]. Kim KJ, et al. PI3K-targeting strategy using alpelisib to enhance the antitumor effect of paclitaxel in human gastric cancer. Sci Rep. 2020;10(1):12308. Published 2020 Jul 23. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Alpelisib (GMP) Related Classifications
HY-15244G Related Classifications
Powered by Bioz