Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Alpelisib [1217486-61-7]

Imprimer

Référence HY-15244-10mg

Conditionnement : 10mg

Marque : MedChemExpress

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Description

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^[1]^[2]^[3]^[4].

IC₅₀ & Target^[1]^[2]

p110α

5 nM (IC₅₀)

p110γ

250 nM (IC₅₀)

p110δ

290 nM (IC₅₀)

p110β

1200 nM (IC₅₀)

p110α-H1047R

4 nM (IC₅₀)

p110α-E545K

4 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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	0.43 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	0.6 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	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]
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]
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	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]
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]
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	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: 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	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	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	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]
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	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	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]
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	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	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	2.3 μM Compound: 1; BYL-719	Antiproliferative activity against human T47D cells Antiproliferative activity against human T47D cells	[PMID: 37652098]
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]

In Vitro

Alpelisib (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 (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 (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 (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 (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 Proliferation Assay^[3]

Cell Line:	MG63, HOS, POS-1, MOS-J
Concentration:	10, 20, 30, 40, 50 μM
Incubation Time:	72 hours
Result:	Inhibited the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with IC₅₀s of 6-15 µM and with IC₉₀s of 24-42 µM.

Cell Cycle Analysis^[3]

Cell Line:	MG63, HOS, POS-1, MOS-J
Concentration:	25 μM
Incubation Time:	18 hours
Result:	Induced a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell .

In Vivo

Alpelisib (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 (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 (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:	A 5-week-old female Rj:NMRI-nude mice with human HOS-MNNG osteosarcoma cells; A 5-week-old male C57Bl/6J mice with mouse MOS-J osteosarcoma cells^[3]
Dosage:	12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice
Administration:	Oral administration; daily; 22 or 29 days for C57Bl/6J mice or Rj:NMRI-nude mice
Result:	Significantly reduced tumor volumes and simultaneously reduced tumor growth.

Animal Model:	Female Sprague Dawley rats ^[1]
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	I.V.
Result:	t_1/2=2.9±0.2 hours.

Essai clinique

Masse moléculaire

441.47

Formule

C₁₉H₂₂F₃N₅O₂S

CAS No.

1217486-61-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(N=C(S1)NC(N2CCC[C@H]2C(N)=O)=O)=C1C3=CC(C(C)(C(F)(F)F)C)=NC=C3

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 83.33 mg/mL (188.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2652 mL	11.3258 mL	22.6516 mL
5 mM	0.4530 mL	2.2652 mL	4.5303 mL
10 mM	0.2265 mL	1.1326 mL	2.2652 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (22.65 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 1% CMC/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (22.65 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.95%

Fiche technique (284 KB) SDS (393 KB)

COA (252 KB) HNMR (191 KB) LCMS (139 KB) Elemental Analysis Report (110 KB)

Instruction de manipulation (2659 KB)

Références

[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 [1217486-61-7]

Référence HY-15244-10mg

Marque : MedChemExpress

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