Alpelisib (BYL719)

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  
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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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 NX;j[mh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\jVlAvOS1zMECg{txO Mn7tO|IhcA>? M4f3bmlEPTB;MT6xNEDPxE1? NXvCephqOjV3NUC1OFk>
SNU-1076 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1GzdFAvOS1zMECg{txO NHLx[Io4OiCq NVjjPHR1UUN3ME22MlgzKM7:TR?= NXrnT5hEOjV3NUC1OFk>
SNU-1066 NH3lVIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vUe|AvOS1zMECg{txO NH;uV|U4OiCq NXr6cVI4UUN3ME2xMlE{KM7:TR?= MmDZNlU2PTB3NEm=
FaDu NUT5WGF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLabmFEOC5zLUGwNEDPxE1? MVS3NkBp MWDJR|UxRTF7Lk[2JO69VQ>? MVyyOVU2ODV2OR?=
SNU1041 NF7pd5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjRNE4yNTFyMDFOwG0> MYm3NkBp Mm\3TWM2OD1{MD62OUDPxE1? NFH5Z40zPTV3MEW0PS=>
SCC25 NEH6dIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljjNE4yNTFyMDFOwG0> NFjOOYY4OiCq M1G4W2lEPTB;NEmuN|Ah|ryP NVnsUZJCOjV3NUC1OFk>
BON-1 NHLTUlVHfW6ldHnvckBCe3OjeR?= NGTqWZQyNzFyIN88US=> NILDd4o1KGh? NEH6SnZqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NETEdlUzPTB{NkK5Ni=>
QGP-1 NIXYXVJHfW6ldHnvckBCe3OjeR?= MXWxM|ExKM7:TR?= NVz5U|I{PCCq NHnaNIlqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NH3nc2QzPTB{NkK5Ni=>
MG-63 NYL5fFIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPTcHdxUUN3ME22JO69Ve,:jDDJR|kxRTJ2IN88US=> M2XlR|I1QTZzN{mw
HOS M4X2bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV75dWxSUUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0> M4LxSFI1QTZzN{mw
MOS-J NVLzc|dHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\2N2FKSzVyPUGwJO69Ve,:jDDJR|kxRTN4IN88US=> MYKyOFk3OTd7MB?=
POS-1 M3nMbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3f0VmlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= NUDyTJI1OjR7NkG3PVA>
92.1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVS1NFAuOjByMDDuUS=> M4jBUVUh\A>? MUnpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> NHrWSYozPDV4M{W0NC=>
Mel270 NGS0dnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljiOVAxNTJyMECgcm0> MV:1JIQ> MknubY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MoPGNlQ2PjN3NEC=
Omm1.3 NX[4UVlGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:1NFAuOjByMDDuUS=> NETRVo82KGR? M{PDV4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M3TvblI1PTZ|NUSw
Omm1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXS1NFAuOjByMDDuUS=> NET0W242KGR? NGrT[Y5qdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? NXf0WnV2OjR3NkO1OFA>
C918 MknQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHLSog2ODBvMkCwNEBvVQ>? MXm1JIQ> NUDDOXZocW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? MXuyOFU3OzV2MB?=
Mel290 NGe2dnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HmSFUxOC1{MECwJI5O M3r2NlUh\A>? NWe1eZg2cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NVPRUI9TOjR3NkO1OFA>
OPM2 NHvmXo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLrNE42NTJwNTFOwG0> MV20PEBp MnfGbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{ToflI1PDB3MUKx
OPM1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGwMlUuOi53IN88US=> NVOwfJRyPDhiaB?= NGHOPYlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mn[4NlQ1ODVzMkG=
U266 NXTPWnpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2O1WlAvPS1{LkWg{txO M2LHR|Q5KGh? NEPNd3pqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGrtTlQzPDRyNUGyNS=>
MM1R MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWP2fZlnOC53LUKuOUDPxE1? NInQc5Q1QCCq M4foOYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NILJWYQzPDRyNUGyNS=>
MM1S M2P6Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfI[VcxNjVvMj61JO69VQ>? NHPZdY41QCCq NEK1SYZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYe5[4dkOjR2MEWxNlE>
H929 NW\tV3BRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorsNE42NTJwNTFOwG0> M{LHWVQ5KGh? M2nmSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVKyOFQxPTF{MR?=
RPMI M4m3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfaSVZ4OC53LUKuOUDPxE1? MX:0PEBp MmS0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWKyOFQxPTF{MR?=
SKBR3 M1;EfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrHN|Mh|ryP NFW0RlI2KGR? NH3wco9qdmirYnn0d{A{Pe,:hTDj[YxtKGe{b4f0bC=> Mn\ONlM6OTh5OUe=
MDA453 NXPGR4NvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDTSZk{OyEQvF2= MmLqOUBl NH75b2NqdmirYnn0d{A{QO,:hTDj[YxtKGe{b4f0bC=> NInqTGkzOzlzOEe5Oy=>
EFM192A M3TtdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoW1N|Mh|ryP NF7XOlE2KGR? NUS5[2E4cW6qaXLpeJMhOjgxvJWgZ4VtdCCpcn;3eIg> Mn7zNlM6OTh5OUe=
AU565 NXzpNI85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYizN{DPxE1? MkjVOUBl MYDpcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= Mmj0NlM6OTh5OUe=
MDA361 NGLsdGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorkN|Mh|ryP M3zSfVUh\A>? NH3VU|FqdmirYnn0d{A1PO,:hTDj[YxtKGe{b4f0bC=> NWTqO|FxOjN7MUi3PVc>
BT474 M4PQbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;qblM{KM7:TR?= NIjwS|Q2KGR? M3XlVIlvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To MXqyN|kyQDd7Nx?=
HCC202 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\FTlM{KM7:TR?= M1mySFUh\A>? M{PFeYlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To NWHabFRJOjN7MUi3PVc>
KPL4 NULiVZNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHriN5Y{OyEQvF2= MlntOUBl MV7pcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= NF\6UGkzOzlzOEe5Oy=>
NCL-N87 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV72XIxqOzNizszN M4HXNVUh\A>? MVfpcohq[mm2czCzNg+9jSClZXzsJIdzd3e2aB?= NYTKXFZ{OjN7MUi3PVc>
UACC812 NWTjSZZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWzN{DPxE1? MYO1JIQ> MYXpcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NIDqUJMzOzlzOEe5Oy=>
HCC2218 MlvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fZb|M{KM7:TR?= NF24Zlc2KGR? M{LpV4lvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To NGS3VnozOzlzOEe5Oy=>
HCC1569 NIj0fIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nxSFM{KM7:TR?= NITnfGo2KGR? MVvpcohq[mm2czC189yGKGOnbHyg[5Jwf3Sq NFriPIszOzlzOEe5Oy=>
OE19 NXzE[oFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKzN{DPxE1? NW\STpJPPSCm MV\pcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= MWmyN|kyQDd7Nx?=
OE33 M1rYWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKzN{DPxE1? MX61JIQ> MVjpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= NUHWdVV1OjN7MUi3PVc>
JIMT1 M2e0Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1ThXFM{KM7:TR?= MlrrOUBl MX7pcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MkjuNlM6OTh5OUe=
HCC1954 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4L2R|M{KM7:TR?= M2H6V|Uh\A>? MXLpcohq[mm2czCyPg+9jSClZXzsJIdzd3e2aB?= NYj6OVg{OjN7MUi3PVc>
NUGC4 M17QUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;lN|Mh|ryP NVTqWGJ{PSCm NGPQUZNqdmirYnn0d{AyPO,:hTDj[YxtKGe{b4f0bC=> Ml;wNlM6OTh5OUe=
ZR-75-30 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnRXppKOzNizszN M4HFbVUh\A>? MUnpcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= Mn30NlM6OTh5OUe=

... 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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PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID