Alpelisib (BYL719)

For research use only. Not for use in humans.

目录号:S2814 中文名称:阿培利司

Alpelisib (BYL719) Chemical Structure

CAS No. 1217486-61-7

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。

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客户使用Selleck生产的Alpelisib (BYL719)发表文献101篇:

产品安全说明书

PI3K抑制剂选择性比较

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
PI3Kα [1]
(Cell-free assay)
5 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Detroit562 NV;TXXBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITneFcxNjFvMUCwJO69VQ>? NYD6RnROPzJiaB?= MV7JR|UxRTFwMUCg{txO NUTq[nVbOjV3NUC1OFk>
SNU-1076 NHvOVHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWwMlEuOTByIN88US=> NXfCeGdFPzJiaB?= NXHEdW9DUUN3ME22MlgzKM7:TR?= MVuyOVU2ODV2OR?=
SNU-1066 NH6zeYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoqxNE4yNTFyMDFOwG0> MXe3NkBp NXTscWFIUUN3ME2xMlE{KM7:TR?= NV6yNFlXOjV3NUC1OFk>
FaDu NHr4XJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPTTHUxNjFvMUCwJO69VQ>? M1\xPVczKGh? NUDIcpFJUUN3ME2xPU43PiEQvF2= NY\yUIJSOjV3NUC1OFk>
SNU1041 MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPem1JOC5zLUGwNEDPxE1? MX23NkBp MofCTWM2OD1{MD62OUDPxE1? M1W2N|I2PTVyNUS5
SCC25 NEHae3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMlEuOTByIN88US=> Mm\DO|IhcA>? NHXRcGlKSzVyPUS5MlMxKM7:TR?= M1TZWlI2PTVyNUS5
BON-1 MYPGeY5kfGmxbjDBd5NigQ>? M3\mNVEwOTBizszN NXLCeIRIPCCq NYrvXWk1cW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= MmXTNlUxOjZ{OUK=
QGP-1 NFXnSpZHfW6ldHnvckBCe3OjeR?= MnT6NU8yOCEQvF2= MnfJOEBp NWS3T3JKcW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= Mk\VNlUxOjZ{OUK=
MG-63 M1jF[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Pqd2lEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= MoWwNlQ6PjF5OUC=
HOS NF21W2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGqwZWFKSzVyPUG1JO69Ve,:jDDJR|kxRTR{IN88US=> MnriNlQ6PjF5OUC=
MOS-J M1vKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzMfIFKSzVyPUGwJO69Ve,:jDDJR|kxRTN4IN88US=> MoWzNlQ6PjF5OUC=
POS-1 M2fUSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\5bHFZUUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> NIXyTYIzPDl4MUe5NC=>
92.1 MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G3TFUxOC1{MECwJI5O MlrvOUBl NFXVVI5qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NWPKTGZOOjR3NkO1OFA>
Mel270 M{jqZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXIdWRSPTByLUKwNFAhdk1? M{Cyd|Uh\A>? NFfDblhqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MXeyOFU3OzV2MB?=
Omm1.3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS1NFAuOjByMDDuUS=> MVW1JIQ> NI\jdW1qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NG\kU2szPDV4M{W0NC=>
Omm1 NIrxdmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXxc3Q2ODBvMkCwNEBvVQ>? M2LuWlUh\A>? NF71TVBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MmTXNlQ2PjN3NEC=
C918 M3TDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXy1NFAuOjByMDDuUS=> Ml63OUBl M1\TVIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M{\5ZlI1PTZ|NUSw
Mel290 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXy1NFAuOjByMDDuUS=> NHTjRlM2KGR? M2LndIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M2L0V|I1PTZ|NUSw
OPM2 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonTNE42NTJwNTFOwG0> MYC0PEBp NUj1dY5qcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NVrO[mZXOjR2MEWxNlE>
OPM1 NV3obGpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfFNE42NTJwNTFOwG0> M4\HOVQ5KGh? NXq2SllCcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYKyOFQxPTF{MR?=
U266 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rKb|AvPS1{LkWg{txO MUW0PEBp MnvxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWOyOFQxPTF{MR?=
MM1R M4HIN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3hNVBkOC53LUKuOUDPxE1? NH7KSpk1QCCq NYT2UnR3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3:2elI1PDB3MUKx
MM1S NYHBPItoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn4b3AxNjVvMj61JO69VQ>? MX60PEBp MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkTvNlQ1ODVzMkG=
H929 M3G0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXewMlUuOi53IN88US=> M2LWXVQ5KGh? M{HGXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYWyOFQxPTF{MR?=
RPMI MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLFNZZyOC53LUKuOUDPxE1? NXviR4s4PDhiaB?= NIXsN3BqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MkO1NlQ1ODVzMkG=
SKBR3 NIT2eFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH30V2o{OyEQvF2= MV21JIQ> MljObY5pcWKrdIOgN|XwxIViY3XscEBoem:5dHi= MVmyN|kyQDd7Nx?=
MDA453 NX7CenBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6zN{DPxE1? M1fINlUh\A>? Mnu5bY5pcWKrdIOgN|jwxIViY3XscEBoem:5dHi= Mnz1NlM6OTh5OUe=
EFM192A NFvROWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HUUFM{KM7:TR?= Ml\2OUBl Mn;qbY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= MXiyN|kyQDd7Nx?=
AU565 M33n[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLXN|Mh|ryP MVS1JIQ> NYHzUFZ6cW6qaXLpeJMhOjcxvJWgZ4VtdCCpcn;3eIg> M1PmUFI{QTF6N{m3
MDA361 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LpTVM{KM7:TR?= MV21JIQ> MVfpcohq[mm2czC0OQ+9jSClZXzsJIdzd3e2aB?= M1[zUlI{QTF6N{m3
BT474 NX3iTW1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLaVpdZOzNizszN NEXNWVg2KGR? M1TiU4lvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To NYm3VGkzOjN7MUi3PVc>
HCC202 NIfhRmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXBN|Mh|ryP M3;UXlUh\A>? M3nyfIlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To NVHj[FBmOjN7MUi3PVc>
KPL4 M2D0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX2zN{DPxE1? MVK1JIQ> MlS4bY5pcWKrdIOgOVjwxIViY3XscEBoem:5dHi= NYfUPVFwOjN7MUi3PVc>
NCL-N87 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILSUnc{OyEQvF2= M17ZbVUh\A>? MY\pcohq[mm2czCzNg+9jSClZXzsJIdzd3e2aB?= M3\2fVI{QTF6N{m3
UACC812 M3zP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LwUlM{KM7:TR?= Mof1OUBl M1:0NolvcGmkaYTzJFI497zHIHPlcIwh\3Kxd4To M1XXT|I{QTF6N{m3
HCC2218 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWzN{DPxE1? MX:1JIQ> MnfmbY5pcWKrdIOgNVXwxIViY3XscEBoem:5dHi= NVzjTmMxOjN7MUi3PVc>
HCC1569 M4n2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ruZ|M{KM7:TR?= NX7PSmtPPSCm NWr3OY91cW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=> NX:zXHlNOjN7MUi3PVc>
OE19 NHTKeodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYmzN{DPxE1? NVjifWc5PSCm NYD4VG0ycW6qaXLpeJMhOjQxvJWgZ4VtdCCpcn;3eIg> M3XNOVI{QTF6N{m3
OE33 NEPn[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrYOGZFOzNizszN MWW1JIQ> MmXHbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= MmHxNlM6OTh5OUe=
JIMT1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfjN|Mh|ryP NETIU|Y2KGR? NWrjOlgzcW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=> M2W5[lI{QTF6N{m3
HCC1954 Mn;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XDVlM{KM7:TR?= NF\nXVI2KGR? M{LT[4lvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To M1:wR|I{QTF6N{m3
NUGC4 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOzN{DPxE1? M1rKflUh\A>? NGHMOVFqdmirYnn0d{AyPO,:hTDj[YxtKGe{b4f0bC=> NGPFTFMzOzlzOEe5Oy=>
ZR-75-30 NVTrc5lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3hN|Mh|ryP NEX3ZWo2KGR? M4jxN4lvcGmkaYTzJE0yPe,:hTDj[YxtKGe{b4f0bC=> MmPMNlM6OTh5OUe=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT(S473) / p-AKT(T308); 

PubMed: 25544637     


PIK3CA hot-spot mutant cell lines were treated with 1 µM BYL719 for the indicated period of time. Lysates were immunoblotted to detect the indicated proteins.

p100β / p110α / p85 / p-ERBB3(Y1289); 

PubMed: 25544637     


BT474 cells were treated with 1 µM BYL719 alone for different durations of time and lysates were immunoprecipitated with ERBB3 antibody. Precipitates were analyzed by western blot with the indicated antibodies.

p-HER2 / IGF-1R; 

PubMed: 25544637     


Cells were treated with 1 μM BYL719 for 24 hr and lysates were immunoblotted to detect the indicated proteins.

pS6 (Ser235-236); 

PubMed: 27048245     


Immunoblots of lysates from parental and resistant cells treated for 24 hours as indicated.

PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD; 

PubMed: 27604488     


T47D cells cultured to resistance in the presence of BYL719. Both parental (T47D) and resistant (T47DR) cells were treated with BYL719 at 1μM, and cell lysates were prepared at 0, 4, 24 hours for immunoblotting for the indicated proteins.

25544637 27048245 27604488
Growth inhibition assay
Cell viability; 

PubMed: 27602501     


The effect of BYL719 on cellular viability was evaluated in HCT116 (A) and SW480 (B) CRC cells. Briefly, cells were grown, treated with increasing concentrations of BYL719 (5, 10 and 20 μM) and cellular viability determined by MTS assay 72h after treatments. Controls included cells that remained untreated (media ctrl) and vehicle-treated controls (DMSO). Data represent means ± SEM of at least triplicate experiments normalized to controls. All conditions were compared with DMSO. Ctrl, control; DMSO, dimethyl sulfoxide. **, p< 0.01; ***, p< 0.001; ****, p< 0.0001.

27602501
Immunofluorescence
LC3; 

PubMed: 26637440     


SKBR3 GFP-LC3 cells were cultured for 5 days with DMSO, 500 nM BKM120 or 500 nM BYL719. Cells were treated with DMSO or 1 μM Lapatinib for the final 18 h. GFP-LC3 localization was captured by fluorescent microscopy.

26637440
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 88 mg/mL (199.33 mM)
Ethanol 2 mg/mL (4.53 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
4.4 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 441.47
化学式

C19H22F3N5O2S

CAS号 1217486-61-7
储存条件 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04524000 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis October 1 2020 Phase 2
NCT04526470 Not yet recruiting Drug: Alpelisib + Paclitaxel Solid Tumor|Stomach Cancer Seoul National University Bundang Hospital September 1 2020 Phase 1|Phase 2
NCT04300790 Not yet recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis June 30 2020 Phase 2
NCT04251533 Recruiting Drug: alpelisib|Drug: placebo|Drug: nab-paclitaxel Triple Negative Breast Neoplasms Novartis Pharmaceuticals|Novartis June 8 2020 Phase 3

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操作手册

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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID