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。

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客户使用Selleck该产品发表文献9篇:

客户使用该产品的3个实验数据:

  • AN3CA (B), JHUEM2 (D), and MFE296 (H) cells were treated with the indicated doses of BGJ398 and BYL719 alone or in combination for 96 hours, and an SRB assay was subsequently performed.

    Mol Cancer Ther, 2017, 16(4):637-648. Alpelisib (BYL719) purchased from Selleck.

    BYL719 induces Apoptosis in MM cells. The effect of increasing concentrations of BYL719 (0-2.5 umol/l) for 48 h on the apoptosis of MM1s cells. The effect of BYL719 on the apoptosis signalling; cleaved PARP, caspase 3, caspase 9 by Western blotting. MM, multple myeloma.

    Br J Haematol 2014 165(1), 89-101. Alpelisib (BYL719) purchased from Selleck.

  • A549 cell was trypsinized and plated at 50% confluence in DMEM. 16 hours later, BYL719 was added at final concentrations of 0, 1, 5, 10 and 20uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- AKT, pS473-AKT, pT286-CyclinD1 and beta-actin (internal control) antibodies.

    Alpelisib (BYL719) purchased from Selleck.

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 M4jEc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\hNFAvOS1zMECg{txO Mn\DO|IhcA>? M1e1cGlEPTB;MT6xNEDPxE1? M333eVI2PTVyNUS5
SNU-1076 M3;aTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37XeVAvOS1zMECg{txO NEj3Wlc4OiCq NVW0OJNYUUN3ME22MlgzKM7:TR?= NXu1e41vOjV3NUC1OFk>
SNU-1066 NIr5[VNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHny[XUxNjFvMUCwJO69VQ>? MluxO|IhcA>? NH;r[nhKSzVyPUGuNVMh|ryP MXyyOVU2ODV2OR?=
FaDu NUj4W|RLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX2wMlEuOTByIN88US=> MX[3NkBp M1PC[mlEPTB;MUmuOlYh|ryP Ml2wNlU2PTB3NEm=
SNU1041 NXzMWoZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[wMlEuOTByIN88US=> M2PnWFczKGh? MnntTWM2OD1{MD62OUDPxE1? Ml7GNlU2PTB3NEm=
SCC25 M1TKb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDkVoQxNjFvMUCwJO69VQ>? MonqO|IhcA>? M3ruO2lEPTB;NEmuN|Ah|ryP NHXVem8zPTV3MEW0PS=>
BON-1 NWPPcVFPTnWwY4Tpc44hSXO|YYm= NEHRNWEyNzFyIN88US=> NV\qRYNiPCCq M2O0SolvcGmkaYTzJHBKO0tiKFHLWEBU\XJ|MEipJIFv\CCvVF;SR|EwOiCjY4Tpeol1cWW| NFziVYYzPTB{NkK5Ni=>
QGP-1 Mk\XSpVv[3Srb36gRZN{[Xl? NW\TUmtnOS9zMDFOwG0> NXrMZ2VDPCCq NFHJ[2NqdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= M3jXRVI2ODJ4Mkmy
MG-63 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofqTWM2OD14IN88Ug+9lCCLQ{mwQVI1KM7:TR?= NV\xbYFZOjR7NkG3PVA>
HOS MlzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPjbXBKSzVyPUG1JO69Ve,:jDDJR|kxRTR{IN88US=> MUSyOFk3OTd7MB?=
MOS-J NVLU[Y5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH20UnVKSzVyPUGwJO69Ve,:jDDJR|kxRTN4IN88US=> MXmyOFk3OTd7MB?=
POS-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TMbWlEPTB;ODFOwG3wxIxiSVO5NF0{PiEQvF2= Mkj2NlQ6PjF5OUC=
92.1 M2fEeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4POSlUxOC1{MECwJI5O NXK1W2lmPSCm M3TN[YlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NYO5NlJ[OjR3NkO1OFA>
Mel270 MlTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7MOVAxNTJyMECgcm0> NH3y[XU2KGR? NXXa[FBxcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M{LmSlI1PTZ|NUSw
Omm1.3 NHPn[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE[3TlU2ODBvMkCwNEBvVQ>? NYm0SZRQPSCm MlOzbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> MmDXNlQ2PjN3NEC=
Omm1 NEjITlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;HRog2ODBvMkCwNEBvVQ>? NFX1TVU2KGR? M3rmXIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NXj4WWkxOjR3NkO1OFA>
C918 M4PyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL2blc2ODBvMkCwNEBvVQ>? MUO1JIQ> NXjwNIJtcW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? M3vHdFI1PTZ|NUSw
Mel290 NHPaS4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi1bItlPTByLUKwNFAhdk1? NF;HNlg2KGR? M1rrPYlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO NGfKc28zPDV4M{W0NC=>
OPM2 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHne3UxNjVvMj61JO69VQ>? NUjwOJJvPDhiaB?= NXLrbohEcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYmyOFQxPTF{MR?=
OPM1 M1focGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3NZZYxNjVvMj61JO69VQ>? NUn5[GJPPDhiaB?= M{\5TYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnjZNlQ1ODVzMkG=
U266 M3n1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe4bJYxNjVvMj61JO69VQ>? NIW0Znk1QCCq M3\tOolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2jVdVI1PDB3MUKx
MM1R MnLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKwMlUuOi53IN88US=> NEjoeWg1QCCq MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4i3dVI1PDB3MUKx
MM1S M2i1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXSNE42NTJwNTFOwG0> M3rBXlQ5KGh? MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlLwNlQ1ODVzMkG=
H929 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TsTVAvPS1{LkWg{txO M2TCRlQ5KGh? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NX75XnJmOjR2MEWxNlE>
RPMI MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPnfWwxNjVvMj61JO69VQ>? NFjx[W81QCCq M1vQNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1jSZVI1PDB3MUKx
SKBR3 NVXMUYMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTqWJVNOzNizszN M3m3OFUh\A>? M1zMZ4lvcGmkaYTzJFM297zHIHPlcIwh\3Kxd4To MWCyN|kyQDd7Nx?=
MDA453 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4iyXFM{KM7:TR?= NHPBOIk2KGR? MVvpcohq[mm2czCzPQ+9jSClZXzsJIdzd3e2aB?= NI\mRnAzOzlzOEe5Oy=>
EFM192A MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;XXZFIOzNizszN NXnHb2FjPSCm MmjybY5pcWKrdIOgNlfwxIViY3XscEBoem:5dHi= M2fCd|I{QTF6N{m3
AU565 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWzN{DPxE1? M2rje|Uh\A>? MU\pcohq[mm2czCyOw+9jSClZXzsJIdzd3e2aB?= MknzNlM6OTh5OUe=
MDA361 M17nUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvqWpM{OzNizszN MUC1JIQ> MonibY5pcWKrdIOgOFTwxIViY3XscEBoem:5dHi= M{S0SVI{QTF6N{m3
BT474 NELiWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnm[|NKOzNizszN M2H6[lUh\A>? NGDJNmpqdmirYnn0d{AyPu,:hTDj[YxtKGe{b4f0bC=> NYX3dnJQOjN7MUi3PVc>
HCC202 NIGycGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rW[|M{KM7:TR?= MmS0OUBl M4LidYlvcGmkaYTzJFIx97zHIHPlcIwh\3Kxd4To NVjCOndSOjN7MUi3PVc>
KPL4 NW\QfXl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDnN|Mh|ryP MWi1JIQ> MUPpcohq[mm2czC1PQ+9jSClZXzsJIdzd3e2aB?= NXrZeHhZOjN7MUi3PVc>
NCL-N87 NVrZVWdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU[3VmZjOzNizszN M4fRW|Uh\A>? NV\DRWhwcW6qaXLpeJMhOzIxvJWgZ4VtdCCpcn;3eIg> MY[yN|kyQDd7Nx?=
UACC812 NW\DU3M5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvuN|Mh|ryP Mn3vOUBl NGDlUoNqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> M3T5c|I{QTF6N{m3
HCC2218 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUSzN{DPxE1? MlXHOUBl M3fv[YlvcGmkaYTzJFE297zHIHPlcIwh\3Kxd4To Mm\1NlM6OTh5OUe=
HCC1569 NFPZV4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorLN|Mh|ryP NF;CW5Q2KGR? NV;j[W5xcW6qaXLpeJMhPe,:hTDj[YxtKGe{b4f0bC=> MWeyN|kyQDd7Nx?=
OE19 NXjuNmlNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjFNYM{OyEQvF2= NHnveJU2KGR? NHnNXIJqdmirYnn0d{AzO+,:hTDj[YxtKGe{b4f0bC=> NUDqTVJMOjN7MUi3PVc>
OE33 NYLlNlY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDZN|Mh|ryP NUT6fXNsPSCm MYHpcohq[mm2czCyN-+9jSClZXzsJIdzd3e2aB?= M4XwbVI{QTF6N{m3
JIMT1 NHK5dmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2j0fVM{KM7:TR?= NHzGZXc2KGR? MV;pcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MXiyN|kyQDd7Nx?=
HCC1954 NVrkV29{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL0eFZUOzNizszN NYP6eYQ6PSCm M{ntRYlvcGmkaYTzJFI697zHIHPlcIwh\3Kxd4To MkPKNlM6OTh5OUe=
NUGC4 MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Pp[lM{KM7:TR?= NIracGs2KGR? MYHpcohq[mm2czCxOQ+9jSClZXzsJIdzd3e2aB?= NV6xemJMOjN7MUi3PVc>
ZR-75-30 M2j3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3SWJQ{OyEQvF2= M2n1UFUh\A>? MX7pcohq[mm2czCtNVXwxIViY3XscEBoem:5dHi= NGXx[GkzOzlzOEe5Oy=>

... Click to View More Cell Line Experimental Data

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
稳定性 powder
in solvent
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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. March 31 2019 Phase 1
NCT03207529 Not yet recruiting Malignant Neoplasm of Breast M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc. March 31 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03631953 Not yet recruiting Meningioma Assistance Publique Hopitaux De Marseille January 1 2019 Phase 1
NCT03601507 Recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) December 14 2018 Phase 2
NCT03601507 Recruiting CDKN2A-p16 Positive|Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma|Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7|Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7|Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 University of Arizona|National Cancer Institute (NCI) December 14 2018 Phase 2

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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