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Alpelisib

Catalog No. T1921 CAS 1217486-61-7

Synonyms: BYL-719

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity. Alpelisib inhibits PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib has antitumor activity and is targeted to PIK3CA mutant tumors.

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Alpelisib, CAS 1217486-61-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 66.00
25 mg	In stock	$ 79.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 156.00
200 mg	In stock	$ 279.00
500 mg	In stock	$ 471.00
1 g	In stock	$ 688.00
1 mL * 10 mM (in DMSO)	In stock	$ 55.00

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Purity: 99.73%

Purity: 99.62%

Purity: 99.25%

Purity: 99.07%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity. Alpelisib inhibits PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib has antitumor activity and is targeted to PIK3CA mutant tumors.
Targets&IC50	p110α:5 nM (cell free), p110γ:250 nM (cell free)
In vitro	METHODS: Osteosarcoma cell lines MG-63, HOS, MOS-J and POS-1 were treated with Alpelisib (0-50 µM) for 72 h and cell viability was measured using XTT assay. RESULTS: Alpelisib significantly inhibited cell growth of all osteosarcoma cell lines in a dose-dependent manner with IC50 ranging from 6-15 µM and IC90 ranging from 24-42 µM. [1] METHODS: PIK3CA wild-type cells (SNU638 and SNU668) and three PIK3CA mutant cells (SNU601, AGS, and MKN1) were treated with Alpelisib (5 µM) for 24 h, and cell cycle profiles were examined using Flow cytometry. RESULTS: Alpelisib treatment induced G0/G1 cell cycle arrest regardless of PIK3CA mutation status. In PIK3CA mutant cells (AGS and MKN1), there was a significant increase in the sub-G1 fraction, suggesting that Alpelisib increased apoptosis in these cell lines. [2]
In vivo	METHODS: To assay anti-tumor activity in vivo, Alpelisib (12.5-50 mg/kg, methylcellulose 0.5%) was administered orally to Rj:NMRI-nude mice bearing human osteosarcoma HOS-MNNG once daily for twenty-two days. RESULTS: Alpelisib significantly reduced tumor volume in a dose-dependent manner. [1] METHODS: To investigate the modulatory effects on collagen, Alpelisib (12.5-50 mg/kg) was administered orally to nude mice bearing subcutaneous xenografts of Rat1-myr-p110α tumors once daily for eight days. RESULTS: Treatment with 12.5, 25, and 50 mg/kg of Alpelisib was well tolerated and produced dose-dependent and statistically significant antitumor effects with a T/C of 14.1% and regressions of 9.6% and 65.2%, respectively. [3]
Cell Research	To evaluate the isoform-specific potency of NVP-BYL719 in a cell-based system, an N-terminally myristoylated form of each PI3K class IA isoform was expressed in Rat1 fibroblasts. The retroviral expression plasmid pBabePuro containing human p110α, p110β, and p110δ with an N-terminal myristoylation (myr) signal followed by an HA-tag were generated. Successfully infected Rat1 cells were selected in medium containing 4 μg/mL of puromycin, expanded and characterized for expression of the p110 isoforms. Transgenic expression of the myristoylated protein was confirmed by increased levels of phosphorylated Akt [1].
Animal Research	All in life experimentation and efficacy studies were conducted as described previously. Tumor xenografts were grown subcutaneously or orthotopically in nude mice or nude Rowett rats (Hsd: RH-Fox1rnu) by injection of 3 × 10^6 to 1 × 10^7 cells or implantation of tumor fragments of approximately 50 mg. Tumor-bearing animals mice were treated with either vehicle control, NVP-BYL719, or NVP-BKM120 (p.o., every day) at the doses indicated [1].

Synonyms	BYL-719
Molecular Weight	441.47
Formula	C19H22F3N5O2S
CAS No.	1217486-61-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 82 mg/mL (185.7 mM)

Ethanol: 2 mg/mL (4.53 mM)

References and Literature

1. Gobin B, et al. BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma. Int J Cancer. 2015 Feb 15;136(4):784-96. 2. Kim KJ, et al. PI3K-targeting strategy using alpelisib to enhance the antitumor effect of paclitaxel in human gastric cancer. Sci Rep. 2020 Jul 23;10(1):12308. 3. Fritsch C, et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther. 2014 May;13(5):1117-29. 4. Elkabets M, et al. mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. Sci Transl Med. 2013 Jul 31;5(196):196ra99. 5. Yang T, Xu R, Su Q, et al. Chelerythrine hydrochloride inhibits proliferation and induces mitochondrial apoptosis in cervical cancer cells via PI3K/BAD signaling pathway[J]. Toxicology in Vitro. 2020, 68: 104965. 6. Liao W, Wang Z, Han Y, et al. Design, synthesis and biological activity of novel 2, 3, 4, 5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity[J]. European Journal of Medicinal Chemistry. 2020: 112309.

Citations

1. Liao W, Wang Z, Han Y, et al. Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity. European Journal of Medicinal Chemistry. 2020, 197: 112309 2. Yang T, Xu R, Su Q, et al. Chelerythrine hydrochloride inhibits proliferation and induces mitochondrial apoptosis in cervical cancer cells via PI3K/BAD signaling pathway. Toxicology in Vitro. 2020, 68: 104965. 3. Chen R, Wang Z, Sima L, et al.Design, synthesis and evaluation of 2, 6, 8-substituted Imidazopyridine derivatives as potent PI3K α inhibitors.Journal of Enzyme Inhibition and Medicinal Chemistry.2023, 38(1): 2155638. 4. Sugawara T, Nevedomskaya E, Heller S, et al.Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis.Molecular Oncology.2024

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library FDA-Approved Kinase Inhibitor Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Bioactive Compound Library

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Keywords

Alpelisib 1217486-61-7 PI3K/Akt/mTOR signaling PI3K Inhibitor Phosphoinositide 3-kinase inhibit phosphorylation p110α cancer antineoplastic AKT BYL719 metastasis mutant BYL 719 PIK3CA breast BYL-719 inhibitor

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