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Alpelisib hydrochloride

Name: Alpelisib hydrochloride
Brand: TargetMol
SKU: T14191
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14191Cas No. 1584128-91-5

Alias BYL 719 hydrochloride

Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent PI3Kα inhibitor (IC₅₀ = 5 nM) with selectivity and oral bioavailability, exhibiting activity against PI3Kβ/γ/δ that is dozens of times weaker than against PI3Kα (IC₅₀ = 250/290/1200 nM). Alpelisib exhibits targeting activity against PIK3CA-mutated tumors and may be utilized in cancer research.

Alpelisib hydrochloride

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Purity: 97.64%

Catalog No. T14191Alias BYL 719 hydrochlorideCas No. 1584128-91-5

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	-	In Stock
5 mg	$48	-	In Stock
10 mg	$64	-	In Stock
25 mg	$82	-	In Stock
50 mg	$98	-	In Stock
100 mg	$156	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:97.64%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent PI3Kα inhibitor (IC₅₀ = 5 nM) with selectivity and oral bioavailability, exhibiting activity against PI3Kβ/γ/δ that is dozens of times weaker than against PI3Kα (IC₅₀ = 250/290/1200 nM). Alpelisib exhibits targeting activity against PIK3CA-mutated tumors and may be utilized in cancer research.
In vitro	Alpelisib hydrochloride (BYL-719) potently inhibits the two most common PIK3CA somatic mutations (H1047R, E545K), with an IC₅₀ of approximately 4 nM. Alpelisib hydrochloride can robustly suppress the phosphorylation level of protein kinase B (Akt) in PI3Kα-transfected cells, with an IC₅₀ of 74±15 nM; in contrast, its inhibitory activity is significantly reduced in cells transfected with the PI3Kβ or PI3Kδ isoform, showing a ≥15-fold decrease compared with that in PI3Kα-transfected cells [2]. Alpelisib hydrochloride (0–50 μM, 72 h) exerts a dose-dependent inhibitory effect on the proliferation of human osteosarcoma cell lines MG63, HOS, POS-1, and MOS-J [3]. Alpelisib hydrochloride (25 μM, 18 h) induces G₀/G₁ phase cell cycle arrest in both human and murine osteosarcoma cell lines [3].
In vivo	Alpelisib hydrochloride (BYL-719) was administered orally at varying doses daily, with 12.5 mg/kg and 50 mg/kg doses for C57Bl/6J mice and 50 mg/kg for female Rj:NMRI nude mice, significantly reducing tumour volume and decreasing the deposition of bone matrix at the parazacco spilurus subsp. spilurus site [3]. Following intravenous injection of 1 mg/kg Alpelisib hydrochloride in rats, the terminal elimination half-life of the drug was moderate, at 2.9 ± 0.2 hours [1].
Synonyms	BYL 719 hydrochloride

Chemical Properties

Molecular Weight	477.93
Formula	C₁₉H₂₃ClF₃N₅O₂S
Cas No.	1584128-91-5
Smiles	CC1=C(C=2C=C(C(C(F)(F)F)(C)C)N=CC2)SC(NC(=O)N3[C@H](C(N)=O)CCC3)=N1.Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (167.39 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0924 mL	10.4618 mL	20.9236 mL	104.6178 mL
5 mM	0.4185 mL	2.0924 mL	4.1847 mL	20.9236 mL
10 mM	0.2092 mL	1.0462 mL	2.0924 mL	10.4618 mL
20 mM	0.1046 mL	0.5231 mL	1.0462 mL	5.2309 mL
50 mM	0.0418 mL	0.2092 mL	0.4185 mL	2.0924 mL
100 mM	0.0209 mL	0.1046 mL	0.2092 mL	1.0462 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc