Alpelisib (Synonyms:BYL-719)
目录号 : KM7765 CAS No. : 1217486-61-7 纯度 : 98%

Alpelisib (BYL-719) 是有效,选择性的,具有口服活性的 PI3Kα 抑制剂。Alpelisib (BYL-719) 对 PIK3CA 突变癌具有靶向性。Alpelisib (BYL-719) 抑制 p110α、p110γ、p110δ、p110β 的 IC50 分别为 5 nM,250 nM,290 nM,1200 nM。具有抗肿瘤活性。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock

Other Forms of Rapamycin:

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生物活性

Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.

体外研究

Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50s~4 nM). Alpelisib potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74±15 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα).
Alpelisib (BYL-719, 0-50 μM; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-dependent manner.
Alpelisib (BYL-719) significantly alters the distribution of cell cycle phases. Alpelisib (BYL-719, 25 μM; 18 hours) induces a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell lines.

Cell Proliferation Assay

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

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 .
体内研究

Alpelisib (BYL-719) (12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes and deposition of ectopic bone matrix.
Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv) .

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
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
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: I.V.
Result: t1/2=2.9±0.2 hours.
分子式
C19H22F3N5O2S
分子量
441.47
CAS号
1217486-61-7
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (188.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5% MC  0.5% Tween-80

    Solubility: 10 mg/mL (22.65 mM); Suspension solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 1% CMC  0.5% Tween-80

    Solubility: 10 mg/mL (22.65 mM); Suspension solution; Need ultrasonic

  • 3.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 5 mg/mL (11.33 mM); Clear solution

  • 4.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.71 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.71 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 5.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 6.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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