Alpelisib (BYL719)
中文名称：阿培利司
Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。
Alpelisib (BYL719) Chemical Structure
CAS: 1217486-61-7
产品质控
批次：
纯度：
99.96%
99.96
Alpelisib (BYL719)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| H929 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| MM1S | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| MM1R | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| U266 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| OPM1 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| OPM2 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| Mel290 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| C918 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| Omm1 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| Omm1.3 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| Mel270 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| 92.1 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| QGP-1 | Function Assay | 1/10 μM | 4 h | inhibits PI3K (AKT Ser308) and mTORC1/2 activities | 25026292 |
| BON-1 | Function Assay | 1/10 μM | 4 h | inhibits PI3K (AKT Ser308) and mTORC1/2 activities | 25026292 |
| SCC25 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=49.30 μM | 25550549 |
| SNU1041 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=20.65 μM | 25550549 |
| FaDu | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=19.66 μM | 25550549 |
| SNU-1066 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=1.13 μM | 25550549 |
| SNU-1076 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=6.82 μM | 25550549 |
| Detroit562 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=1.10 μM | 25550549 |
| RPMI | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| SKBR3 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 35％ cell growth | 23918797 |
| MDA453 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 38％ cell growth | 23918797 |
| EFM192A | Growth Inhibition Assay | 33 μM | 5 d | inhibits 27％ cell growth | 23918797 |
| AU565 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 26％ cell growth | 23918797 |
| MDA361 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 44％ cell growth | 23918797 |
| BT474 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 16％ cell growth | 23918797 |
| HCC202 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 20％ cell growth | 23918797 |
| KPL4 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 58％ cell growth | 23918797 |
| NCL-N87 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 31％ cell growth | 23918797 |
| UACC812 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 27％ cell growth | 23918797 |
| HCC2218 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 15％ cell growth | 23918797 |
| HCC1569 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 5％ cell growth | 23918797 |
| OE19 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 23％ cell growth | 23918797 |
| OE33 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 23％ cell growth | 23918797 |
| JIMT1 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 9％ cell growth | 23918797 |
| HCC1954 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 29％ cell growth | 23918797 |
| NUGC4 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 14％ cell growth | 23918797 |
| ZR-75-30 | Growth Inhibition Assay | 33 μM | 5 d | inhibits -15％ cell growth | 23918797 |
| POS-1 | Growth Inhibition Assay | IC50=8 μM， IC90=36 μM | 24961790 | ||
| MOS-J | Growth Inhibition Assay | IC50=10 μM， IC90=36 μM | 24961790 | ||
| HOS | Growth Inhibition Assay | IC50=15 μM， IC90=42 μM | 24961790 | ||
| MG-63 | Growth Inhibition Assay | IC50=6 μM， IC90=24 μM | 24961790 | ||
| Rat1 | P110alpha inhibition assay | IC50 = 0.074 μM | 26164189 | ||
| Rat1 | PI3Kalpha inhibition assay | IC50 = 0.074 μM | 26206504 | ||
| Rat1 | P110alpha inhibition assay | IC50 = 0.074 μM | 23726034 | ||
| Rat1 | P110delta inhibition assay | IC50 = 1.2 μM | 26164189 | ||
| Rat1 | PI3Kgamma inhibition assay | IC50 = 1.2 μM | 26206504 | ||
| Rat1 | P110delta inhibition assay | IC50 = 1.2 μM | 23726034 | ||
| Rat1 | P110beta inhibition assay | IC50 = 2.2 μM | 26164189 | ||
| Rat1 | PI3Kbeta inhibition assay | IC50 = 2.2 μM | 26206504 | ||
| Rat1 | P110alpha inhibition assay | IC50 = 2.2 μM | 23726034 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | BYL719抑制含有PIK3CA突变体的乳腺癌细胞系的增殖，与PI3K/Akt通路各种下游信号组分的抑制相关。[1] |
|||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AKT(S473) / p-AKT(T308) p100β / p110α / p85 / p-ERBB3(Y1289) p-HER2 / IGF-1R pS6 (Ser235-236) PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD |
|
25544637 | |
| Growth inhibition assay | Cell viability |
|
27602501 | |
| Immunofluorescence | LC3 |
|
26637440 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | BYL719(>270 mg/d)在PIK3CA突变体异种移植啮齿动物模型中表现出统计学显著的剂量依赖性抗肿瘤效能。BYL719具有低清除率，半衰期为8.5小时，并且它的作用在30mg/d 和450mg/d之间剂量成比例的增加，在人的Cmax 和AUC中显示出低的个体差异。BYL719(270mg/d)首次表现出临床疗效的迹象，包括在ER+乳腺癌患者中证实的部分响应，以及17个患者中8个实现了显著的PET响应(PMR)和/或肿瘤治愈。[1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05948943 | Recruiting | Lymphatic Malformations |
Novartis Pharmaceuticals|Novartis |
November 24 2023 | Phase 2|Phase 3 |
| NCT05660083 | Recruiting | HER2-negative Breast Cancer|Metastatic Breast Cancer|Metaplastic Breast Carcinoma|TNBC - Triple-Negative Breast Cancer |
The Methodist Hospital Research Institute|Novartis Pharmaceuticals |
January 12 2023 | Phase 2 |
| NCT05508906 | Recruiting | Metastatic Breast Cancer|Advanced Breast Cancer|HR-positive Breast Cancer|HER2-negative Breast Cancer |
Olema Pharmaceuticals Inc.|Novartis |
August 31 2022 | Phase 1 |
| NCT05230810 | Recruiting | HER2-positive Metastatic Breast Cancer |
Criterium Inc.|Novartis|Seagen Inc. |
August 25 2022 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 441.47 | 分子式 | C19H22F3N5O2S |
| CAS号 | 1217486-61-7 | SDF | Download Alpelisib (BYL719) SDF |
| Smiles | CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 88 mg/mL ( (199.33 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
Tags: buy Alpelisib (BYL719) | Alpelisib (BYL719) supplier | purchase Alpelisib (BYL719) | Alpelisib (BYL719) cost | Alpelisib (BYL719) manufacturer | order Alpelisib (BYL719) | Alpelisib (BYL719) distributor
