Tamanho : 5mg
Synonyms: BYL-719
| Description | Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors. |
| Targets & IC50 | p110δ:290 nM, p110α:5 nM (cell free), p110γ:250 nM (cell free), p110α-E545K:4 nM, p110α-H1047R:4 nM, p110β:1200 nM |
| In vitro | Method: 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. Result: 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] Method: 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. Result: 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 | Method: 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. Result: Alpelisib significantly reduced tumor volume in a dose-dependent manner. [1] Method: 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. Result: 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] |
| Synonyms | BYL-719 |
| 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]. |
| Molecular Weight | 441.47 |
| Formula | C19H22F3N5O2S |
| Cas No. | 1217486-61-7 |
| Smiles | O=C(N1[C@H](C(N)=O)CCC1)NC2=NC(C)=C(C3=CC(C(C)(C)C(F)(F)F)=NC=C3)S2 |
| Relative Density. | 1.391 g/cm3 |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 240 mg/mL (543.64 mM), Sonication is recommended.  Ethanol: 2 mg/mL (4.53 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (22.65 mM), Solution. 10% DMSO+90% Saline: < 10 mg/mL (22.65 mM), insoluble. Lower concentrations may be soluble, but exact solubility limit is unknown. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO 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.
1) Add 100 μL of the DMSO 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 and mix thoroughly until a homogeneous solution is obtained.
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