Alpelisib (BYL719)

For research use only. Not for use in humans.

目录号:S2814

Alpelisib (BYL719) Chemical Structure

Molecular Weight(MW): 441.47

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 4864.29 现货
RMB 3034.22 现货
RMB 4650.12 现货
RMB 7115.91 现货
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客户使用Selleck生产的Alpelisib (BYL719)发表文献54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 Mk\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPpNE4yNTFyMDFOwG0> MonHO|IhcA>? MW\JR|UxRTFwMUCg{txO MVOyOVU2ODV2OR?=
SNU-1076 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnsXYxyOC5zLUGwNEDPxE1? NG\aO2M4OiCq MkTaTWM2OD14LkiyJO69VQ>? MXyyOVU2ODV2OR?=
SNU-1066 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XoS|AvOS1zMECg{txO NYi5[oFnPzJiaB?= NVS0SHlYUUN3ME2xMlE{KM7:TR?= MV6yOVU2ODV2OR?=
FaDu NY\COHJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzySZAxNjFvMUCwJO69VQ>? NWDPcWVbPzJiaB?= MUXJR|UxRTF7Lk[2JO69VQ>? MVKyOVU2ODV2OR?=
SNU1041 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DrbFAvOS1zMECg{txO MofTO|IhcA>? NHPLO4JKSzVyPUKwMlY2KM7:TR?= MX2yOVU2ODV2OR?=
SCC25 M36ySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKwMlEuOTByIN88US=> MofQO|IhcA>? NWnjW3FDUUN3ME20PU4{OCEQvF2= MnXENlU2PTB3NEm=
BON-1 Mn[5SpVv[3Srb36gRZN{[Xl? NYHJPINkOS9zMDFOwG0> MXW0JIg> NVm2fJV{cW6qaXLpeJMhWEl|SzCoRWtVKFOnckOwPEkh[W6mIH3UU3JEOS9{IHHjeIl3cXSrZYO= M3X6ZVI2ODJ4Mkmy
QGP-1 MlyzSpVv[3Srb36gRZN{[Xl? MUexM|ExKM7:TR?= MmfaOEBp NE[5T4ZqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= MlTSNlUxOjZ{OUK=
MG-63 NYD4bndPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:1RWNKSzVyPU[g{txO97zOIFnDPVA:OjRizszN Mn\FNlQ6PjF5OUC=
HOS Mki2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{WzdGlEPTB;MUWg{txO97zOIFnDPVA:PDJizszN NH:1SVQzPDl4MUe5NC=>
MOS-J M{P5U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVewbY1zUUN3ME2xNEDPxE4xvJygTWM6OD1|NjFOwG0> M{HUN|I1QTZzN{mw
POS-1 Mo\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7CTnhKSzVyPUig{txO97zOIFnDPVA:OzZizszN Ml\uNlQ6PjF5OUC=
92.1 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXG4PJJYPTByLUKwNFAhdk1? NV\we3R3PSCm M2TyVIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO MkP3NlQ2PjN3NEC=
Mel270 M4HKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PvNlUxOC1{MECwJI5O NWHWNGlPPSCm NV\OOmlKcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NUXLTXJtOjR3NkO1OFA>
Omm1.3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3TOVAxNTJyMECgcm0> NYqxNWFXPSCm MU\pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NWfhU2pGOjR3NkO1OFA>
Omm1 NYLuW4hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvicGszPTByLUKwNFAhdk1? NHzFT4M2KGR? M1HaU4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M1z1e|I1PTZ|NUSw
C918 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX21NFAuOjByMDDuUS=> M1TzWlUh\A>? NF;BRoFqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? MVmyOFU3OzV2MB?=
Mel290 NH7sUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXZXI82ODBvMkCwNEBvVQ>? MWW1JIQ> MYLpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NFX1dnQzPDV4M{W0NC=>
OPM2 NVTrZVM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\XNE42NTJwNTFOwG0> NWHweopsPDhiaB?= NY\lelAycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYqyOFQxPTF{MR?=
OPM1 MoPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3i0VFAvPS1{LkWg{txO NYHTTnR6PDhiaB?= MUDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MofYNlQ1ODVzMkG=
U266 NXrueJFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDkNE42NTJwNTFOwG0> MW[0PEBp MmTYbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUT6S3l{OjR2MEWxNlE>
MM1R MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3roOVAvPS1{LkWg{txO NFqxVJU1QCCq M3Kye4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NH:yWGkzPDRyNUGyNS=>
MM1S NVWyRWx{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\PdHlLOC53LUKuOUDPxE1? NHjMO201QCCq M3fqfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1jrNlI1PDB3MUKx
H929 MnTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\qdYZmOC53LUKuOUDPxE1? NWfhSplrPDhiaB?= NVLGXpZPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MoHINlQ1ODVzMkG=
RPMI NEXpd2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSwMlUuOi53IN88US=> MXO0PEBp M1TKPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoTTNlQ1ODVzMkG=
SKBR3 M2\Q[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\WW5g{OyEQvF2= MWm1JIQ> NFjve45qdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=> MUSyN|kyQDd7Nx?=
MDA453 NYOwTo5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:zN{DPxE1? M2PPdFUh\A>? NWLubXB[cW6qaXLpeJMhOzkxvJWgZ4VtdCCpcn;3eIg> MkD0NlM6OTh5OUe=
EFM192A NX:wWXdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGzN{DPxE1? M{DVV|Uh\A>? NVT3[pBbcW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> MY[yN|kyQDd7Nx?=
AU565 NH61eY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\zZlE{OyEQvF2= NGXyWZI2KGR? NH75cVBqdmirYnn0d{AzPu,:hTDj[YxtKGe{b4f0bC=> NIW3eogzOzlzOEe5Oy=>
MDA361 MmntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXIUYk{OyEQvF2= NF[2OGo2KGR? MUfpcohq[mm2czC0OQ+9jSClZXzsJIdzd3e2aB?= NEDsd4QzOzlzOEe5Oy=>
BT474 M4PPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLuN|Mh|ryP NHrHOnI2KGR? MUHpcohq[mm2czCxOw+9jSClZXzsJIdzd3e2aB?= NY\ZbG1UOjN7MUi3PVc>
HCC202 NEf0XHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfJb3o5OzNizszN MoDpOUBl MlHibY5pcWKrdIOgNlDwxIViY3XscEBoem:5dHi= M1fnSlI{QTF6N{m3
KPL4 NEHxcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W3clM{KM7:TR?= M1zmSFUh\A>? MVzpcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= NEn2PIszOzlzOEe5Oy=>
NCL-N87 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DMTFM{KM7:TR?= M3H6O|Uh\A>? NF7WUlJqdmirYnn0d{A{Oe,:hTDj[YxtKGe{b4f0bC=> NHTTVFEzOzlzOEe5Oy=>
UACC812 MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW[zN{DPxE1? MX61JIQ> NYHEN2xocW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> NGXrTY4zOzlzOEe5Oy=>
HCC2218 NFKwbI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHkc|JUOzNizszN NWrYeXJIPSCm M4nGe4lvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To Mn;GNlM6OTh5OUe=
HCC1569 M{fjNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S5eVM{KM7:TR?= NFzxXIY2KGR? NUfw[2RLcW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=> MkDjNlM6OTh5OUe=
OE19 NHf5cZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzOfnN2OzNizszN M3vH[|Uh\A>? M3fzT4lvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To M3u4eFI{QTF6N{m3
OE33 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzxRYc{OyEQvF2= NYfuSXRqPSCm MoTjbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= M2exblI{QTF6N{m3
JIMT1 M2XXdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfFSFlVOzNizszN MmT4OUBl NV7HO3lRcW6qaXLpeJMhQe,:hTDj[YxtKGe{b4f0bC=> NWLlOpVEOjN7MUi3PVc>
HCC1954 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVyzN{DPxE1? MlKzOUBl MWTpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= MVuyN|kyQDd7Nx?=
NUGC4 NUPOTIloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rySVM{KM7:TR?= MWe1JIQ> MXTpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= MYSyN|kyQDd7Nx?=
ZR-75-30 NWH3R|VVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjRfVI{OyEQvF2= MmS2OUBl NHj1PHNqdmirYnn0d{AuOTYxvJWgZ4VtdCCpcn;3eIg> MUiyN|kyQDd7Nx?=

... 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):
30% PEG400+0.5% Tween80+5% propylene glycol
30 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

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
NCT03207529 Recruiting Drug: Alpelisib|Drug: Enzalutamide Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Androgen Receptor Positive|Estrogen Receptor Negative|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Progesterone Receptor Negative|Progesterone Receptor Positive|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|PTEN Positive|Recurrent Breast Carcinoma|Refractory Breast Carcinoma|Triple-Negative Breast Carcinoma M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Novartis|Astellas Pharma Global Development Inc. June 7 2019 Phase 1
NCT02620839 Recruiting Drug: Alpelisib|Drug: Cisplatin Solid Tumors Pamela Munster|University of California San Francisco December 1 2016 Phase 1
NCT02734615 Recruiting Drug: LSZ102|Drug: LEE011|Drug: BYL719 Advanced or Metastatic ER+ Breast Cancer Novartis Pharmaceuticals|Novartis June 14 2016 Phase 1
NCT02550743 Terminated Drug: BYL719|Drug: Capecitabine|Radiation: Radiation Rectal Cancer howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) June 3 2016 Phase 1
NCT02437318 Active not recruiting Drug: Fulvestrant|Drug: Alpelisib|Drug: Alpelisib placebo Breast Cancer Novartis Pharmaceuticals|Novartis July 23 2015 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