Cat. No.: HY-15244G

Alpelisib (GMP)

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.

For research use only. We do not sell to patients.

CAS No.: 1217486-61-7
Formula: C₁₉H₂₂F₃N₅O₂S
Molecular Weight:441.47

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Alpelisib (GMP) Chemical Structure

CAS No.: 1217486-61-7

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 5 nM (p110α), 250 nM (p110γ), 290 nM (p110δ), 1200 nM (p110β)^[1]

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	4 μM Compound: 1	Antiproliferative activity against human A549 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
AGS	IC₅₀	0.52 μM Compound: Alpelisib	Antiproliferative activity against human AGS cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human AGS cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]
DU-145	IC₅₀	4 μM Compound: 1	Antiproliferative activity against human DU-145 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human DU-145 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
HCT-116	IC₅₀	3.73 μM Compound: 1	Antiproliferative activity against human HCT-116 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
HGC-27	IC₅₀	1.92 μM Compound: Alpelisib	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]
HT-29	IC₅₀	1.94 μM Compound: 1	Antiproliferative activity against human HT-29 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human HT-29 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
Kasumi 1	IC₅₀	0.44 μM Compound: Alpelisib	Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 37126967]
L-363	IC₅₀	0.26 μM Compound: 1; BYL-719	Antiproliferative activity against human L-363 cells Antiproliferative activity against human L-363 cells	[PMID: 37652098]
L-363	IC₅₀	0.17 μM Compound: Alpelisib	Antiproliferative activity against human L-363 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human L-363 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 39605166]
LNCaP	IC₅₀	15.8 μM Compound: Alpelisib	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]
MCF7	IC₅₀	530 nM Compound: 2; BYL719	Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay	[PMID: 33356246]
MCF7	IC₅₀	0.43 μM Compound: Alpelisib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
MCF7	IC₅₀	0.25 μM Compound: 1; BYL-719	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 37652098]
MCF7	IC₅₀	0.6 μM Compound: Alpelisib	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 7 days by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 7 days by CCK8 assay	[PMID: 39159497]
MCF7	IC₅₀	1.2 μM Compound: Alpelisib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 39605166]
MCF7	IC₅₀	3.34 μM Compound: 1	Antiproliferative activity against human MCF7 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
MDA-MB-231	IC₅₀	62.9 μM Compound: Alpesilib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
MDA-MB-231	IC₅₀	3.12 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
MDA-MB-453	IC₅₀	0.77 μM Compound: Alpelisib	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]
MGC-803	IC₅₀	0.43 μM Compound: Alpelisib	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35834807]
MV4-11	IC₅₀	3.5 μM Compound: Alpelisib	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38048697]
MV4-11	IC₅₀	0.19 μM Compound: Alpelisib	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of chidamide by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs in presence of chidamide by CCK-8 assay	[PMID: 38048697]
NCI-H446	IC₅₀	0.68 μM Compound: 1	Antiproliferative activity against human NCI-H446 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human NCI-H446 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
PC-3	IC₅₀	3.53 μM Compound: 1	Antiproliferative activity against human PC-3 cells incubated for 96 hrs by MTT assay Antiproliferative activity against human PC-3 cells incubated for 96 hrs by MTT assay	[PMID: 40047238]
PC-3	IC₅₀	13.19 μM Compound: Alpelisib	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]
Pfeiffer	IC₅₀	50 μM Compound: Alpelisib	Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]
Rat1	IC₅₀	1.2 μM Compound: 8, NVP-BYL719	Inhibition of N-terminal myristoylated P110delta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA Inhibition of N-terminal myristoylated P110delta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA	[PMID: 23726034]
Rat1	IC₅₀	2.2 μM Compound: 8, NVP-BYL719	Inhibition of N-terminal myristoylated P110beta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA Inhibition of N-terminal myristoylated P110beta (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA	[PMID: 23726034]
Rat1	IC₅₀	0.074 μM Compound: 8, NVP-BYL719	Inhibition of N-terminal myristoylated P110alpha (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA Inhibition of N-terminal myristoylated P110alpha (unknown origin)-mediated AKT phosphorylation at Ser473 expressed in rat Rat1 cells by ELISA	[PMID: 23726034]
Rat1	IC₅₀	0.074 μM Compound: 1, BYL719	Inhibition of myristoylated human P110alpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis Inhibition of myristoylated human P110alpha expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis	[PMID: 26164189]
Rat1	IC₅₀	2.2 μM Compound: 1, BYL719	Inhibition of myristoylated human P110beta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis Inhibition of myristoylated human P110beta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis	[PMID: 26164189]
Rat1	IC₅₀	1.2 μM Compound: 1, BYL719	Inhibition of myristoylated human P110delta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis Inhibition of myristoylated human P110delta expressed in Rat1 cells assessed as inhibition of Akt phosphorylation at Serine 473 by Western blot analysis	[PMID: 26164189]
Rat1	IC₅₀	0.074 μM Compound: Alpelisib	Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serum Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serum	[PMID: 26206504]
Rat1	IC₅₀	2.2 μM Compound: Alpelisib	Inhibition of PI3Kbeta in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serum Inhibition of PI3Kbeta in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serum	[PMID: 26206504]
Rat1	IC₅₀	1.2 μM Compound: Alpelisib	Inhibition of PI3Kgamma in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serum Inhibition of PI3Kgamma in rat Rat1 cells assessed as reduction of Akt phosphorylation at Ser473 in presence of 0.5% fetal calf serum	[PMID: 26206504]
SJRH30	IC₅₀	7.6 μM Compound: BYL719	Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay	[PMID: 33109399]
T47D	IC₅₀	420 nM Compound: 2; BYL719	Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay	[PMID: 33356246]
T47D	IC₅₀	0.1 μM Compound: Alpelisib	Antiproliferative activity against human T47D cells expressing PIK3CA mutant assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human T47D cells expressing PIK3CA mutant assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 37126967]
T47D	IC₅₀	2.3 μM Compound: 1; BYL-719	Antiproliferative activity against human T47D cells Antiproliferative activity against human T47D cells	[PMID: 37652098]
T47D	IC₅₀	0.4 μM Compound: Alpelisib	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 7 days by CCK8 assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 7 days by CCK8 assay	[PMID: 39159497]
T47D	IC₅₀	0.36 μM Compound: Alpelisib	Antiproliferative activity against human T47D cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay Antiproliferative activity against human T47D cells assessed as inhibition of cell viability incubated for 3 days by MTT/CTG assay	[PMID: 40518729]

In Vitro

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 Viability Assay^[1]

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 Proliferation Assay^[2]

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).

Apoptosis Analysis^[2]

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.

Western Blot Analysis^[2]

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 Differentiation Assay^[2]

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.

In Vivo

Alpelisib GMP (50 mg/kg; i.p.; daily) exerts partial antitumor activity against alpelisib-resistant MCF7R breast cancer xenografts, with maximum efficacy achieved when combined with SGK3 knockdown^[3].
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
Molecular Weight 441.47
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]

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Alpelisib (GMP)

All PI3K Isoforms