Alpelisib hydrochloride (Synonyms: BYL-719 hydrochloride)

Name: Alpelisib hydrochloride
Brand: MedChemExpress
SKU: HY-15244A
Rating: 5.0 (125 reviews)

Cat. No.: HY-15244A Purity: 99.55%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Alpelisib (BYL-719) hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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. : 1584128-91-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 125 publication(s) in Google Scholar

Other Forms of Alpelisib hydrochloride:

Alpelisib In-stock

125 Publications Citing Use of MCE Alpelisib hydrochloride

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Combined Palbociclib- and Fulvestrant-resistant cells, M-S and T-S, and the corresponding resistant cells, MPF-R and TPF-R, were treated with different inhibitors of the PI3K/AKT/mTOR pathway including Alpelisib (HY-15244; Alp; 1 μM in M-S/MPF-R and 250 to 500 nM in T-S/TPF-R), Capivasertib (Cap; 250 to 500 nM in M-S/MPF-R and 100 nM in T-S/TPF-R), Sapanisertib (Sap; 10 nM in M-S/MPF-R and 5 nM in T-S/TPF-R), and Gedatolisib (HY-10681; Ged; 10 nM) in combination with Palbociclib (HY-50767; Palbo; 200 nM) and Fulvestrant (HY-13636; Fulv; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Combined Palbociclib- and Fulvestrant-resistant cells (wild type ER+ breast cancer cells), ZPF-R, and the corresponding sensitive cells, Z-S, were treated with different inhibitors of PI3K/AKT/mTOR including Alpelisib (HY-15244; 6 μM), Capivasertib (50 nM), Sapanisertib (5 nM), and Gedatolisib (HY-10681; 5 nM) in combination with Palbociclib (HY-50767; 150 nM) and Fulvestrant (HY-13636; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Triple combination with Gedatolisib (HY-10681), Palbociclib (HY-50767), and Fulvestrant (HY-13636) effectively inhibits growth of PIK3CA-mutant ER+ tumor xenografts resistant to combined palbociclib and fulvestrant. MPF-R cells (1 × 106) resistant to combined palbociclib and fulvestrant were injected into the mammary fat pads of NOG CIEA mice, and tumors were allowed to establish for 2 weeks to a size of ≈30 mm3. Mice were then treated with the combination of Fulvestrant (100 mg/kg, sc weekly), Palbociclib (25 mg/kg, oral gavage daily), and Capivasertib (100 mg/kg, oral gavage daily; n = 6) or Alpelisib (HY-15244; 25 mg/kg, oral gavage daily; n = 5). Tumor size was measured weekly. Average tumor growth curves measured weekly and Tumor volumes measured after excision.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Gedatolisib efficiently reduced the viability of ER+ PIK3CA- or AKT1-mutant breast cancer PDOs resistant to Abemaciclib. Dose-effect curves of CDK4/6i Abemaciclib, dual PI3K/mTORi Gedatolisib (HY-10681), PI3Ki Alpelisib (HY-15244), and dual mTORC1/2i Sapanisertib at day 7 of treatment in three breast cancer PDOs, PDO-P40, PDO-P46, and PDO-P48 (n = 3 biological replicates per group), developed from ER+ breast tumors and selected because of their differing IC50 toward Abemaciclib.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]; Effect of 1 μM Abemaciclib, Gedatolisib (HY-10681), Alpelisib (HY-15244), or Sapanisertib on viability of PDO-P40, PDO-P46, or PDO-P48 during 7 days of treatment. Data are presented as means ± SEM. Significant differences are calculated by one-way ANOVA test (*P < 0.05, **P < 0.01, and ***P < 0.001).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17;9(1):146.; Alpelisib (50 mg/kg; p.o.). Western blot and quantification of P-AKTSer473 and P-S6RP of the skin of PIK3CA^WT and PIK3CA^Tie2-CreER mice treated with either vehicle, rapamycin, miransertib or alpelisib (n = 3–4 per group).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17;9(1):146.; Alpelisib (50 mg/kg; p.o.). Representative immunofluorescence staining of KI67 in the skin of PIK3CA^WT and PIK3CA^Tie2-CreER mice treated with either vehicle, rapamycin, miransertib or alpelisib. Scale bar: 10 μm.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Jun 12;41(6):1103-1117.e12. [Abstract]; Quantification of image-based cell death of organoid lines after 72 h treatment with alpelisib, idelalisib, umbralisib in indicated concentrations (0 as in DMSO vehicle control, 10, 50, and 100 μM) and bortezomib (10 μM, positive control). Cell death is estimated as the percentage of PI-positive cells out of total number of Hoechst 33342-positive nuclei, followed by normalization to the DMSO vehicle control (negative control) and positive control (bortezomib) values.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Nov 1;13(11):2432-2447. [Abstract]; Alpelisib (50 mg/kg q.d.; administered for 3 days in the PK/PD group and 28 days in the efficacy group) reduces pAKT/AKT in the skeletal muscle of mice with CAL-33 (H1047R PI3Kα-mutant) xenograft models.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Nov 1;13(11):2432-2447. [Abstract]; Correlation plot of alpelisib and STX-478 comparing pAKT IC50 at 1 hour and viability [CellTiter-Glo (CTGlo)] GI50 at 72 hours across the indicated panel of cell lines.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 Oct 6;13(614):eabg0809. [Abstract]; Alpelisib (50 mg/kg/day; p.o.; approximately 3 months) inhibits the PI3K/AKT/mTOR pathway in lymphatic tissues of PIK3CA^VEGFR3-CreER mice, reducing phosphorylation levels of AKT and S6RP.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2019 Jan:440-441:54-63. [Abstract]; The siNC- or siBTF3-transfected breast cancer cells are treated with BYL-719 and are then subjected to an immunoblotting analysis.

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2018 Jun;558(7711):540-546. [Abstract]; Western blot of P-AKT (Ser⁴⁷³), P-AKT (Thr³⁰⁸) and P-S6RP in liver, heart and muscles, respectively, from PIK3CA^WT and PIK3CA^CAGG-CreER mice treated with or without BYL719 directly after Cre induction (preventive) or seven days later (therapeutic).

: Alpelisib hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]; (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

In Vitro

Alpelisib hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (10 μM; 4 d) and a 1 μM SGK3 inhibitor (VPS34-IN1 (HY-12795) or SGK3-IN) produces enhanced antiproliferative activity in Alpelisib hydrochloride-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) hydrochloride 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) hydrochloride 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) hydrochloride 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
Result:	Significantly reduced tumor volumes and simultaneously reduced tumor growth.

Animal Model:	Female Sprague Dawley rats ^[1]
Dosage:	1 mg/kg (Pharmacokinetic Study)
Administration:	I.V.
Result:	T_1/2=2.9±0.2 hours.

Molecular Weight

477.93

Formula

C₁₉H₂₃ClF₃N₅O₂S

CAS No.

1584128-91-5

Appearance

Solid

Color

Light yellow to 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.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (209.24 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	2.0924 mL	10.4618 mL	20.9236 mL
5 mM	0.4185 mL	2.0924 mL	4.1847 mL
10 mM	0.2092 mL	1.0462 mL	2.0924 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 5 mg/mL (10.46 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.46 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.55%

Select Batch:

Data Sheet (284 KB) SDS (252 KB)

COA (253 KB) HNMR (144 KB) RP-HPLC (246 KB) LCMS (386 KB)

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.

[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.

[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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0924 mL	10.4618 mL	20.9236 mL	52.3089 mL
	5 mM	0.4185 mL	2.0924 mL	4.1847 mL	10.4618 mL
	10 mM	0.2092 mL	1.0462 mL	2.0924 mL	5.2309 mL
	15 mM	0.1395 mL	0.6975 mL	1.3949 mL	3.4873 mL
	20 mM	0.1046 mL	0.5231 mL	1.0462 mL	2.6154 mL
	25 mM	0.0837 mL	0.4185 mL	0.8369 mL	2.0924 mL
	30 mM	0.0697 mL	0.3487 mL	0.6975 mL	1.7436 mL
	40 mM	0.0523 mL	0.2615 mL	0.5231 mL	1.3077 mL
	50 mM	0.0418 mL	0.2092 mL	0.4185 mL	1.0462 mL
	60 mM	0.0349 mL	0.1744 mL	0.3487 mL	0.8718 mL
	80 mM	0.0262 mL	0.1308 mL	0.2615 mL	0.6539 mL
	100 mM	0.0209 mL	0.1046 mL	0.2092 mL	0.5231 mL

Alpelisib hydrochloride Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alpelisib1584128-91-5BYL-719BYL719BYL 719PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Alpelisib hydrochloride (Synonyms: BYL-719 hydrochloride)

Customer Review

Other Forms of Alpelisib hydrochloride:

Alpelisib hydrochloride Related Antibodies

125 Publications Citing Use of MCE Alpelisib hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Alpelisib hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Alpelisib hydrochloride Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report