Referencia número: HY-15244

Alpelisib

(Synonyms: BYL-719)

130 Cited Publications

Revisión del cliente

Based on 130 publication(s) in Google Scholar

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.88%
No. CAS: 1217486-61-7
Fòrmula: C₁₉H₂₂F₃N₅O₂S
Peso molecular:441.47

Almacenamiento:

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

Alpelisib Chemical Structure

No. CAS: 1217486-61-7

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (130)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Bioz

Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas PI3K :

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1217486-61-7
Appearance Solid
Peso molecular 441.47
Fòrmula C₁₉H₂₂F₃N₅O₂S
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
Synonyms

BYL-719
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (130)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyWBIF

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Signal Transduct Target Ther

Family with sequence similarity 114 member A1 orchestrates immune evasion in triple-negative breast cancer. [Abstract]

2025 Nov 18;10(1):373. PMID: 41249116
Signal Transduct Target Ther

Targeted therapy for capillary-venous malformations. [Abstract]

2024 Jun 17;9(1):146. PMID: 38880808

Alpelisib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17;9(1):146. [Abstract]

Western blot 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 (50 mg/kg; p.o.). (n = 3–4 per group).

Alpelisib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17;9(1):146. [Abstract]

Representative immunofluorescence staining of KI67 in the skin of PIK3CA^WT and PIK3CA^Tie2-CreER mice treated with either vehicle Alpelisib (50 mg/kg; p.o.). Scale bar: 10 μm.
Nature

Targeted therapy in patients with PIK3CA-related overgrowth syndrome. [Abstract]

2018 Jun;558(7711):540-546. PMID: 29899452

Alpelisib 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).
Science

Interpretation of cancer mutations using a multiscale map of protein systems. [Abstract]

2021 Oct;374(6563):eabf3067. PMID: 34591613
Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]

2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026
Cancer Cell

Evolutionary states and trajectories characterized by distinct pathways stratify patients with ovarian high grade serous carcinoma. [Abstract]

2023 Jun 12;41(6):1103-1117.e12. PMID: 37207655

Alpelisib 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.
Cell

Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]

2025 May 29;188(11):3065-3080.e21. PMID: 40393457
J Hematol Oncol

Combination of PI3K and MEK inhibitors yields durable remission in PDX models of PIK3CA-mutated metaplastic breast cancers. [Abstract]

2020 Feb 22;13(1):13. PMID: 32087759
Cancer Discov

STX-478, a Mutant-Selective, Allosteric PI3Ka Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Ka-Mutant Xenografts. [Abstract]

2023 Nov 1;13(11):2432-2447. PMID: 37623743

Alpelisib 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 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.
Cancer Discov

The INPP4B Tumor Suppressor Modulates EGFR Trafficking and Promotes Triple-Negative Breast Cancer. [Abstract]

2020 Aug;10(8):1226-1239. PMID: 32513774
Cell Metab

Fasting-mimicking diet blocks triple-negative breast cancer and cancer stem cell escape. [Abstract]

2021 Nov 2;33(11):2247-2259.e6. PMID: 34731655
Nat Cancer

CDK4/6 inhibition reprograms the breast cancer enhancer landscape by stimulating AP-1 transcriptional activity. [Abstract]

2021 Jan;2(1):34-48. PMID: 33997789
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Blood

Single-cell genomics details the maturation block in BCP-ALL and identifies therapeutic vulnerabilities in DUX4-r cases. [Abstract]

2024 Jul 5:blood.2023021705. PMID: 38968149
Blood

Targeted inhibition of PI3Kα/δ is synergistic with BCL-2 blockade in genetically defined subtypes of DLBCL. [Abstract]

2019 Jan 3;133(1):70-80. PMID: 30322870
Nat Aging

Dietary supplementation of clinically utilized PI3K p110α inhibitor extends the lifespan of male and female mice. [Abstract]

2023 Feb;3(2):162-172. PMID: 37118113
Cancer Res

Genomic Alterations in PIK3CA-Mutated Breast Cancer Result in mTORC1 Activation and Limit the Sensitivity to PI3Kα Inhibitors. [Abstract]

2021 May 1;81(9):2470-2480. PMID: 33685991
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Liver lipophagy ameliorates nonalcoholic steatohepatitis through extracellular lipid secretion. [Abstract]

2023 Jul 13;14(1):4084. PMID: 37443159
Nat Commun

MAPK4 promotes triple negative breast cancer growth and reduces tumor sensitivity to PI3K blockade. [Abstract]

2022 Jan 11;13(1):245. PMID: 35017531
Nat Commun

PLK1 inhibition exhibits strong anti-tumoral activity in CCND1-driven breast cancer metastases with acquired palbociclib resistance. [Abstract]

2020 Aug 13;11(1):4053. PMID: 32792481
Cell Death Differ

p53 transcriptionally activates DCP1B to suppress tumor progression and enhance tumor sensitivity to PI3K blockade in non-small cell lung cancer. [Abstract]

2025 Apr 9. PMID: 40200093
Sci Transl Med

Dual PI3K/mTOR inhibition is required to combat resistance to CDK4/6 inhibitor and endocrine therapy in PIK3CA-mutant breast cancer. [Abstract]

2025 Dec 17;17(829):eadp5088. PMID: 41406241

Alpelisib 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 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 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 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 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).
Sci Transl Med

Alpelisib administration reduced lymphatic malformations in a mouse model and in patients. [Abstract]

2021 Oct 6;13(614):eabg0809. PMID: 34613809

Alpelisib 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.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Clin Invest

WWP1 inactivation enhances efficacy of PI3K inhibitors while suppressing their toxicities in breast cancer models. [Abstract]

2021 Dec 15;131(24):e140436. PMID: 34907909
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
J Nanobiotechnology

Matrix micro/nano-topography drives oncogenic signaling and drug response in a 3D osteosarcoma model. [Abstract]

2026 Mar 6;24(1):345. PMID: 41787498
Sci Adv

PIK3CA gain-of-function mutation in adipose tissue induces metabolic reprogramming with Warburg-like effect and severe endocrine disruption. [Abstract]

2022 Dec 9;8(49):eade7823. PMID: 36490341
Brain

Angiogenic switching in cerebral cavernous malformations driven by MAP3K3-PIK3CA synergy. [Abstract]

2026 Jan 19:awag017. PMID: 41552909
J Exp Med

MYC is a clinically significant driver of mTOR inhibitor resistance in breast cancer. [Abstract]

2023 Nov 6;220(11):e20211743. PMID: 37642941
J Exp Med

Hemifacial myohyperplasia is due to somatic muscular PIK3CA gain-of-function mutations and responds to pharmacological inhibition. [Abstract]

2023 Nov 6;220(11):e20230926. PMID: 37712948
Cancer Lett

Combined inhibition of CDK4/6 and AKT is highly effective against the luminal androgen receptor (LAR) subtype of triple negative breast cancer. [Abstract]

2024 Sep 5:217219. PMID: 39244005
Cancer Lett

FOXK2 amplification promotes breast cancer development and chemoresistance. [Abstract]

2024 Aug 10:597:217074. PMID: 38901667
Mol Psychiatry

CCL5 promotion of bioenergy metabolism is crucial for hippocampal synapse complex and memory formation. [Abstract]

2021 Nov;26(11):6451-6468. PMID: 33931731
Cancer Lett

Inhibition of BTF3 sensitizes luminal breast cancer cells to PI3Kα inhibition through the transcriptional regulation of ERα. [Abstract]

2019 Jan:440-441:54-63. PMID: 30315845

Alpelisib 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.
Cell Death Dis

Reln-Dab1 pathway mitigates retinal ganglion cell apoptosis in retinal ischemia-reperfusion injury. [Abstract]

2025 May 29;16(1):423. PMID: 40442071
Cell Death Dis

A cytosolic mutp53(E285K) variant confers chemoresistance of malignant melanoma. [Abstract]

2023 Dec 14;14(12):831. PMID: 38097548
Cell Death Dis

Focal adhesion kinase plays a dual role in TRAIL resistance and metastatic outgrowth of malignant melanoma. [Abstract]

2022 Jan 12;13(1):54. PMID: 35022419
Cell Death Dis

CD44/HA signaling mediates acquired resistance to a PI3Kα inhibitor. [Abstract]

2020 Oct 6;11(10):831. PMID: 33024087
Proc Natl Acad Sci U S A

PIK3CA gain-of-function mutation in Schwann cells leads to severe neuropathy and aerobic glycolysis through a non-cell autonomous effect. [Abstract]

2025 Jul;122(26):e2424867122. PMID: 40553493
Proc Natl Acad Sci U S A

Cryo-EM structures of cancer-specific helical and kinase domain mutations of PI3Kα. [Abstract]

2022 Nov 16;119(46):e2215621119. PMID: 36343266
EMBO Mol Med

Somatic PIK3R1 mutations in the iSH2 domain are accessible to PI3Kα inhibition. [Abstract]

2025 Jul;17(7):1556-1574. PMID: 40389643
EMBO Mol Med

A novel model of glioblastoma recurrence to identify therapeutic vulnerabilities. [Abstract]

2025 Jun;17(6):1325-1354. PMID: 40295888
NPJ Precis Oncol

Co-clinical trial targeting ER, FGFR and CDK4/6 in resistant hormone-positive breast cancer with FGFR alterations. [Abstract]

2025 Nov 7;9(1):343. PMID: 41203797
Neoplasia

PIK3CA mutant cervical cancer is selectively suppressed by PI3Kα inhibition (Alpelisib/BYL-719 and Inavolisib/GDC-0077) and cooperates with HPV directed T cell therapy. [Abstract]

2026 Jun:76:101305. PMID: 41980433
Neoplasia

P110α inhibitor alpelisib exhibits a synergistic effect with pyrotinib and reverses pyrotinib resistant in HER2+ breast cancer. [Abstract]

2023 Sep:43:100913. PMID: 37348428
Cell Syst

A Multi-center Study on the Reproducibility of Drug-Response Assays in Mammalian Cell Lines. [Abstract]

2019 Jul 24;9(1):35-48.e5. PMID: 31302153
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Diabetes

A Single Dose of Phosphoinositide-3-kinase Inhibitor Alpelisib Induces Insulin Resistance in Healthy Adults: A Randomized Feasibility Study. [Abstract]

2024 Sep 12:db240402. PMID: 39264822
J Transl Med

Metformin counteracts stimulatory effects induced by insulin in primary breast cancer cells. [Abstract]

2022 Jun 7;20(1):263. PMID: 35672854
Biomed Pharmacother

Dual PI3K/mTOR inhibitor PKI-402 suppresses the growth of ovarian cancer cells by degradation of Mcl-1 through autophagy. [Abstract]

2020 Sep;129:110397. PMID: 32585451
Oncogene

Identification of RAPGEF3 as the therapeutic vulnerability of basal-subtype lung squamous cell carcinoma. [Abstract]

2025 Sep;44(34):3142-3148. PMID: 40781157
Oncogene

PI3K-p110α mediates resistance to HER2-targeted therapy in HER2+, PTEN-deficient breast cancers. [Abstract]

2016 Jul 7;35(27):3607-12. PMID: 26500061

Alpelisib 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).
Aging Cell

Aging Reshapes γ/δ T-Cell Immunity Through a Type I Interferon-Foxo1 Axis. [Abstract]

2026 Feb;25(2):e70389. PMID: 41560320
Cell Rep

Epinephrine inhibits PI3Kα via the Hippo kinases. [Abstract]

2023 Dec 26;42(12):113535. PMID: 38060450
Cell Rep

Methylation of the chromatin modifier KMT2D by SMYD2 contributes to therapeutic response in hormone-dependent breast cancer. [Abstract]

2024 May 2;43(5):114174. PMID: 38700982
Cell Rep

IFNα-induced BST2+ tumor-associated macrophages facilitate immunosuppression and tumor growth in pancreatic cancer by ERK-CXCL7 signaling. [Abstract]

2024 Apr 23;43(4):114088. PMID: 38602878
Cell Rep

Divergent Roles of PI3K Isoforms in PTEN-Deficient Glioblastomas. [Abstract]

2020 Sep 29;32(13):108196. PMID: 32997991
J Med Chem

Rational Design of a Novel 6 H-Benzo[ c]chromen Series as Selective PI3Kα Inhibitors. [Abstract]

2024 Sep 12;67(17):15387-15410. PMID: 39159497
Br J Cancer

PAK and PI3K pathway activation confers resistance to KRASG12C inhibitor sotorasib. [Abstract]

2023 Jan;128(1):148-159. PMID: 36319849
Antioxidants

Serine-Driven Metabolic Plasticity Drives Adaptive Resilience in Pancreatic Cancer Cells. [Abstract]

2025 Jul 7;14(7):833. PMID: 40722937
Cell Biosci

Inhibition of PI3 kinase isoform p110α suppresses neuroblastoma growth and induces the reduction of Anaplastic Lymphoma Kinase. [Abstract]

2022 Dec 30;12(1):210. PMID: 36585695
JCI Insight

ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors. [Abstract]

2022 Aug 22;7(16):e155899. PMID: 35852858
Breast Cancer Res

Analysis of genomic and non-genomic signaling of estrogen receptor in PDX models of breast cancer treated with a combination of the PI3K inhibitor alpelisib (BYL719) and fulvestrant. [Abstract]

2021 May 21;23(1):57. PMID: 34020697
Virulence

Neutrophil extracellular trap-borne C3-driven endothelial dysfunction in Klebsiella pneumoniae liver abscess. [Abstract]

2025 Dec;16(1):2580104. PMID: 41146461
Cancer Metab

CD36 inhibition enhances the anti-proliferative effects of PI3K inhibitors in PTEN-loss anti-HER2 resistant breast cancer cells. [Abstract]

2025 Feb 7;13(1):6. PMID: 39920872
Cells

The AGEs/RAGE Transduction Signaling Prompts IL-8/CXCR1/2-Mediated Interaction between Cancer-Associated Fibroblasts (CAFs) and Breast Cancer Cells. [Abstract]

2022 Aug 4;11(15):2402. PMID: 35954247
Int J Mol Sci

An Increase in Mucin2 Expression Is Required for Colon Cancer Progression Mediated by L1. [Abstract]

2023 Aug 30;24(17):13418. PMID: 37686224
Int J Oncol

HepaCAM‑PIK3CA axis regulates the reprogramming of glutamine metabolism to inhibit prostate cancer cell proliferation. [Abstract]

2022 Apr;60(4):37. PMID: 35191516
Int J Mol Sci

Inhibition of Phosphatidylinositol 3-kinase (PI3K) Signaling Synergistically Potentiates Antitumor Efficacy of Paclitaxel and Overcomes Paclitaxel-Mediated Resistance in Cervical Cancer. [Abstract]

2019 Jul 10;20(14):3383. PMID: 31295843
Cancer Nanotechnol

2023 Mar 29.
Biomolecules

Efficacy of Providing the PI3K p110α Inhibitor BYL719 (Alpelisib) to Middle-Aged Mice in Their Diet. [Abstract]

2021 Jan 25;11(2):150. PMID: 33503847
Int J Cancer

Establishment of patient-derived organoids for guiding personalized therapies in breast cancer patients. [Abstract]

2024 Jul 15;155(2):324-338. PMID: 38533706
Biosci Rep

Prolonged treatment with a PI3K p110α inhibitor causes sex- and tissue-dependent changes in antioxidant content, but does not affect mitochondrial function. [Abstract]

2020 Oct 30;40(10):BSR20201128. PMID: 33006363
Mol Cancer Res

PIK3CA and p53 Mutations Promote 4NQO-Initated Head and Neck Tumor Progression and Metastasis in Mice. [Abstract]

2020 Jun;18(6):822-834. PMID: 32152233
RSC Adv

Development, cross-validation and greenness assessment of capillary electrophoresis method for determination of ALP in pharmaceutical dosage forms - an alternative to liquid chromatography. [Abstract]

2024 Oct 18;14(45):32876-32882. PMID: 39429931
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Cancers (Basel)

Designing Organoid Models to Monitor Cancer Progression, Plasticity and Resistance: The Right Set Up for the Right Question. [Abstract]

2022 Jul 22;14(15):3559. PMID: 35892818
Cancers (Basel)

FoxO3a Inhibits Tamoxifen-Resistant Breast Cancer Progression by Inducing Integrin α5 Expression. [Abstract]

2022 Jan 2;14(1):214. PMID: 35008379
Ther Adv Med Oncol

Navitoclax combined with Alpelisib effectively inhibits Merkel cell carcinoma cell growth in vitro. [Abstract]

2020 Dec 14:12:1758835920975621. PMID: 33403016
Gynecol Oncol

A first-in-class CDK4 inhibitor demonstrates in vitro, ex-vivo and in vivo efficacy against ovarian cancer. [Abstract]

2020 Dec;159(3):827-838. PMID: 32958271
Sci Rep

Targeting CB1 and TRPM8 receptors to counteract CD8+ T cell exhaustion. [Abstract]

2026 Apr 10;16(1):16876. PMID: 41963448
Sci Rep

Steroid hormone receptors, exome sequencing and treatment responsiveness of breast cancer patient-derived xenografts originated in a South American country. [Abstract]

2025 Jan 18;15(1):2415. PMID: 39827242
Sci Rep

The role of the PIK3CA gene in the development and aging of the brain. [Abstract]

2021 Jan 11;11(1):291. PMID: 33431926
Oncol Rep

PI3K p110α inhibition sensitizes cervical cancer cells with aberrant PI3K signaling activation to PARP inhibitor BMN673. [Abstract]

2019 Nov;42(5):2097-2107. PMID: 31545455
PNAS Nexus

Oncogenic PIK3CA mutations shape an immunoregulatory microenvironment in mosaic overgrowth disorders. [Abstract]

2026 May 13;5(6):pgag163. PMID: 42222744
Anal Bioanal Chem

Surfactant-enhanced emulsification liquid-liquid microextraction combined with sweeping micellar electrokinetic chromatography-tandem mass spectrometry for therapeutic drug monitoring of alpelisib and fulvestrant in human plasma. [Abstract]

2025 Nov 17. PMID: 41249630
Br J Haematol

Evaluation of the PIK3 pathway in peripheral T-cell lymphoma and NK/T-cell lymphoma. [Abstract]

2020 May;189(4):731-744. PMID: 32004387
Mol Cell Biochem

Bioelectric fields drive pulmonary epithelial proliferation through PI3K/AKT/GSK3β signaling. [Abstract]

2026 Jan 29. PMID: 41609898
Cell Signal

Isoform specific regulation of osteopontin by AKT2 in hepatocytes and livers. [Abstract]

2025 Apr 9:111799. PMID: 40216173
J Proteome Res

TMTpro-18plex: The Expanded and Complete Set of TMTpro Reagents for Sample Multiplexing. [Abstract]

2021 May 7;20(5):2964-2972. PMID: 33900084
Cancer Res Commun

Cooperative Roles of Class IA PI3K Isoforms in Translocation-Related Sarcoma Cell Survival and Proliferation. [Abstract]

2026 Apr 1;6(4):976-993. PMID: 41916029
Front Oncol

Zotatifin, an eIF4A-Selective Inhibitor, Blocks Tumor Growth in Receptor Tyrosine Kinase Driven Tumors. [Abstract]

2021 Nov 24:11:766298. PMID: 34900714
Endocrinology

TRβ Agonism Induces Tumor Suppression and Enhances Drug Efficacy in Anaplastic Thyroid Cancer in Female Mice. [Abstract]

2023 Aug 28;164(10):bqad135. PMID: 37702560
Front Oncol

Patient-Derived Xenograft Models for Intrahepatic Cholangiocarcinoma and Their Application in Guiding Personalized Medicine. [Abstract]

2021 Jul 13:11:704042. PMID: 34327143
Am J Cancer Res

Establishment of patient-derived xenograft models of adenoid cystic carcinoma to assess pre-clinical efficacy of combination therapy of a PI3K inhibitor and retinoic acid. [Abstract]

2021 Mar 1;11(3):773-792. PMID: 33791153
J Anal Sci Technol

13, 31 (2022).
PLoS One

Development of a novel PIK3CA-mutated pancreatic tumor mouse model and evaluation of the therapeutic effects of a PI3K inhibitor. [Abstract]

2025 Jul 10;20(7):e0326491. PMID: 40638603
PLoS One

Development of an in vivo syngeneic mouse transplant model of invasive intestinal adenocarcinoma driven by endogenous expression of Pik3caH1047R and Apc loss. [Abstract]

2024 Aug 2;19(8):e0308051. PMID: 39093890
Cell Biochem Biophys

Isogarcinol Reduces MARS Levels and Deactivates the PI3K/AKT Pathway to Suppress the Malignant Properties of Breast Cancer Cells. [Abstract]

2025 Mar 22. PMID: 40120049
Biochem Biophys Res Commun

Functional characterization of PIK3CA E545A mutation in MCF-7 breast cancer cells reveals enhanced proliferation and resistance to Alpelisib. [Abstract]

2026 Jun 24:829:154189. PMID: 42341421
Biochem Biophys Res Commun

Neutralization of HSF1 in cells from PIK3CA-related overgrowth spectrum patients blocks abnormal proliferation. [Abstract]

2020 Sep 24;530(3):520-526. PMID: 32620236
Cancer Biomark

TUBB3 (βIII-tubulin) drives gastric cancer progression and poor prognosis by regulating cell cycle and invadopodia formation. [Abstract]

2025 Oct;42(10):18758592251390145. PMID: 41129675
Biomed Rep

Inhibition of SGK1 potentiates the anticancer activity of PI3K inhibitor in NSCLC cells through modulation of mTORC1, p‑ERK and β‑catenin signaling. [Abstract]

2023 Oct 13;19(6):94. PMID: 37901878
Am J Transl Res

Undemineralized dentin matrix particles accelerate blood vessel formation in a critical-sized skull defect through activating the TGF-β/PI3K signaling pathway. [Abstract]

2025 Jun 15;17(6):4689-4700. PMID: 40672621
STAR Protoc

Quantification of cell death and proliferation of patient-derived ovarian cancer organoids through 3D imaging and image analysis. [Abstract]

2023 Nov 16;4(4):102683. PMID: 37976153
bioRxiv

Loss of PIK3CA allows in vitro growth but not in vivo progression of KRAS mutant lung adenocarcinoma in a syngeneic orthotopic implantation model. [Abstract]

2026 Feb 4:2026.02.02.701385. PMID: 41676515
bioRxiv

2026 Jan 18.
medRxiv

A Three-subtype Molecular model of Cervical Cancer: Multiple PI3K Pathway inhibitors suppress growth and cooperate with HPV-directed immunotherapy. [Abstract]

2026 Jan 23:2026.01.21.26344562. PMID: 41646800
Technical University of Dresden

2025.
bioRxiv

2025 Dec 5.
bioRxiv

Loss of the tumor suppressor PTEN activates cell-intrinsic interferon signaling to drive immune resistance. [Abstract]

2025 Sep 20:2025.09.17.676669. PMID: 41000885
University of Cologne

2024.
bioRxiv

2024 November 03.
bioRxiv

2024 August 18.
bioRxiv

2024 July 07.
Preprints

2024 Feb 16.
bioRxiv

2023 Aug 22.
bioRxiv

FOXK2 amplification and overexpression promotes breast cancer development and chemoresistance. [Abstract]

2023 May 30:2023.05.28.542643. PMID: 37398114
Research Square Preprint

2023 May 10.
Research Square Preprint

2023 May 9.
Patent

US20220313694A1.
Patent

US20220249511A1.
Research Square Preprint

2022 Jan.
Research Square Preprint

2020 Aug.
bioRxiv

2020 Jan.

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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.

Working Solution

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (284 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2652 mL	11.3258 mL	22.6516 mL	56.6290 mL
	5 mM	0.4530 mL	2.2652 mL	4.5303 mL	11.3258 mL
	10 mM	0.2265 mL	1.1326 mL	2.2652 mL	5.6629 mL
	15 mM	0.1510 mL	0.7551 mL	1.5101 mL	3.7753 mL
	20 mM	0.1133 mL	0.5663 mL	1.1326 mL	2.8314 mL
	25 mM	0.0906 mL	0.4530 mL	0.9061 mL	2.2652 mL
	30 mM	0.0755 mL	0.3775 mL	0.7551 mL	1.8876 mL
	40 mM	0.0566 mL	0.2831 mL	0.5663 mL	1.4157 mL
	50 mM	0.0453 mL	0.2265 mL	0.4530 mL	1.1326 mL
	60 mM	0.0378 mL	0.1888 mL	0.3775 mL	0.9438 mL
	80 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7079 mL
	100 mM	0.0227 mL	0.1133 mL	0.2265 mL	0.5663 mL

Keywords

Alpelisib

130 Cited Publications

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Alpelisib

Anti-Infection Compound Library

Apoptosis Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Anti-COVID-19 Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

FDA Approved & Pharmacopeial Drug Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Therapy Drug Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

Chemotherapy Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

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FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

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Anti-Rheumatic Arthritis Compound Library

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Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Alpelisib

Ver todos los productos específicos de isoformas PI3K

Actividad biológica

Chemical Information

Publications (130)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table