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 NYjvcGJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;ONE4yNTFyMDFOwG0> MVS3NkBp MkHoTWM2OD1zLkGwJO69VQ>? M1TJV|I2PTVyNUS5
SNU-1076 NV3BUlg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPYfJMxNjFvMUCwJO69VQ>? MlX3O|IhcA>? MYfJR|UxRTZwOEKg{txO M4nPcVI2PTVyNUS5
SNU-1066 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XmelAvOS1zMECg{txO MX23NkBp MV3JR|UxRTFwMUOg{txO MmL5NlU2PTB3NEm=
FaDu NUjqV2hCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMlEuOTByIN88US=> NX34[JdKPzJiaB?= NIjt[2pKSzVyPUG5MlY3KM7:TR?= MoS3NlU2PTB3NEm=
SNU1041 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPGZZcxNjFvMUCwJO69VQ>? Mn7uO|IhcA>? NG[0UGRKSzVyPUKwMlY2KM7:TR?= MWKyOVU2ODV2OR?=
SCC25 NV3Ye3hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELx[VExNjFvMUCwJO69VQ>? NX;oO2pQPzJiaB?= MUDJR|UxRTR7LkOwJO69VQ>? NIrGUFAzPTV3MEW0PS=>
BON-1 Mk[2SpVv[3Srb36gRZN{[Xl? MkDkNU8yOCEQvF2= NHTVSXg1KGh? MXTpcohq[mm2czDQTVNMKCiDS2SgV4VzOzB6KTDhcoQhdVSRUlOxM|Ih[WO2aY\peIlmew>? NW\kXWVuOjVyMk[yPVI>
QGP-1 MUDGeY5kfGmxbjDBd5NigQ>? MVuxM|ExKM7:TR?= MoLOOEBp NEPadm5qdmirYnn0d{BRUTONIDjBT3QhW2W{M{C4LUBidmRibWTPVmMyNzJiYXP0bZZqfGmncx?= NFHLbWYzPTB{NkK5Ni=>
MG-63 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fRcGlEPTB;NjFOwG3wxIxiSVO5NF0zPCEQvF2= NIDae3MzPDl4MUe5NC=>
HOS M4fvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTHN4V6UUN3ME2xOUDPxE4xvJygTWM6OD12MjFOwG0> NF3XcXkzPDl4MUe5NC=>
MOS-J NV;ZRo1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFyIN88Ug+9lCCLQ{mwQVM3KM7:TR?= MojiNlQ6PjF5OUC=
POS-1 NVLiUFZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrrdYZqUUN3ME24JO69Ve,:jDDJR|kxRTN4IN88US=> MnfoNlQ6PjF5OUC=
92.1 NVj3Z4FWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTre2FrPTByLUKwNFAhdk1? MmjrOUBl M{LrS4lvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhU\XJ2N{OpJJVxKHSxIEGg{txO M2\QTVI1PTZ|NUSw
Mel270 NGjHZmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zCT|UxOC1{MECwJI5O M3uzdlUh\A>? NX;1SFQ6cW6qaXLpeJMhfGinIIDoc5NxcG:{eXzheIlwdiCxZjDBT3QhMFOnckS3N{khfXBidH:gNUDPxE1? NFexXpEzPDV4M{W0NC=>
Omm1.3 NGXnR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT2OVAxNTJyMECgcm0> M4[wd|Uh\A>? MmXYbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> NY\LSVdlOjR3NkO1OFA>
Omm1 NVf6bZhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:1NFAuOjByMDDuUS=> NYTZSnJMPSCm MV;pcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV4VzPDd|KTD1dEB1dyBzIN88US=> MmHSNlQ2PjN3NEC=
C918 Ml3LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXyOVAxNTJyMECgcm0> M2mweFUh\A>? Mmr5bY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHNmejR5MzmgeZAhfG9iMTFOwG0> Ml61NlQ2PjN3NEC=
Mel290 NVXoSIlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWT4N45SPTByLUKwNFAhdk1? MkPDOUBl NFfPbmVqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApW2W{NEezLUB2eCC2bzCxJO69VQ>? M{fOdVI1PTZ|NUSw
OPM2 M3fsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGD4[FUxNjVvMj61JO69VQ>? NFfRb5c1QCCq NE\Jd3pqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmrTNlQ1ODVzMkG=
OPM1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jL[VAvPS1{LkWg{txO M4fkNlQ5KGh? NU[5N5VTcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3rRU|I1PDB3MUKx
U266 NWrXVGxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjNfmcxNjVvMj61JO69VQ>? Mlf0OFghcA>? M1P1c4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mnr6NlQ1ODVzMkG=
MM1R NGf3bZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnWb5dUOC53LUKuOUDPxE1? M4nLbFQ5KGh? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXzLfZFROjR2MEWxNlE>
MM1S M4n6RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHKbZkxNjVvMj61JO69VQ>? MkTROFghcA>? MXLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXWyOFQxPTF{MR?=
H929 NYDD[pBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTLNE42NTJwNTFOwG0> M2nETFQ5KGh? NFv1N41qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1fNWFI1PDB3MUKx
RPMI M4DaWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHsNE42NTJwNTFOwG0> M1rx[VQ5KGh? MWHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF\IeI8zPDRyNUGyNS=>
SKBR3 M3;4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTncmYzOzNizszN NInnOXM2KGR? MnXNbY5pcWKrdIOgN|XwxIViY3XscEBoem:5dHi= NHXp[IIzOzlzOEe5Oy=>
MDA453 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXezN{DPxE1? NHHFbHA2KGR? M{jnfolvcGmkaYTzJFM597zHIHPlcIwh\3Kxd4To MlSyNlM6OTh5OUe=
EFM192A MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDZUVcyOzNizszN Ml;OOUBl MV;pcohq[mm2czCyO-+9jSClZXzsJIdzd3e2aB?= NIS4SI0zOzlzOEe5Oy=>
AU565 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKzN{DPxE1? MnzsOUBl MmfrbY5pcWKrdIOgNlbwxIViY3XscEBoem:5dHi= NGnUN4ozOzlzOEe5Oy=>
MDA361 NWDs[IczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqzN{DPxE1? MmnwOUBl M4rtSYlvcGmkaYTzJFQ197zHIHPlcIwh\3Kxd4To Mo\PNlM6OTh5OUe=
BT474 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MneyN|Mh|ryP MoT6OUBl M1L3N4lvcGmkaYTzJFE397zHIHPlcIwh\3Kxd4To NGq0U5EzOzlzOEe5Oy=>
HCC202 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYn1fXFDOzNizszN MWG1JIQ> NWjHSI8ycW6qaXLpeJMhOjExvJWgZ4VtdCCpcn;3eIg> MYOyN|kyQDd7Nx?=
KPL4 NUX3NHNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fDfFM{KM7:TR?= NYPTdph2PSCm M3nwUYlvcGmkaYTzJFU597zHIHPlcIwh\3Kxd4To NG[1OmwzOzlzOEe5Oy=>
NCL-N87 NInxWZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITKWHE{OyEQvF2= NGfVVGk2KGR? NHLTPWlqdmirYnn0d{A{Oe,:hTDj[YxtKGe{b4f0bC=> NV;aRlRXOjN7MUi3PVc>
UACC812 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KwU|M{KM7:TR?= MlzVOUBl NEHQ[YtqdmirYnn0d{AzP+,:hTDj[YxtKGe{b4f0bC=> MWeyN|kyQDd7Nx?=
HCC2218 MlzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1i0SVM{KM7:TR?= NEPiPHg2KGR? Mn;sbY5pcWKrdIOgNVXwxIViY3XscEBoem:5dHi= NUfxV5AyOjN7MUi3PVc>
HCC1569 M1j1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr4N|Mh|ryP NUjCbYNwPSCm M{fw[YlvcGmkaYTzJFXwxIViY3XscEBoem:5dHi= M4PXVVI{QTF6N{m3
OE19 NWi3coZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6zN{DPxE1? NFfKWJE2KGR? Ml3mbY5pcWKrdIOgNlPwxIViY3XscEBoem:5dHi= NGm5NnYzOzlzOEe5Oy=>
OE33 NF\yVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfWN|Mh|ryP M2LQW|Uh\A>? M{HKRolvcGmkaYTzJFI{97zHIHPlcIwh\3Kxd4To MonxNlM6OTh5OUe=
JIMT1 NWPNeGlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;UZmQ{OyEQvF2= MnzXOUBl MXvpcohq[mm2czC589yGKGOnbHyg[5Jwf3Sq MWiyN|kyQDd7Nx?=
HCC1954 NF:5TpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmL6N|Mh|ryP M1nGOVUh\A>? NV7OfIdscW6qaXLpeJMhOjoxvJWgZ4VtdCCpcn;3eIg> MUGyN|kyQDd7Nx?=
NUGC4 NGTifXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHFfXdwOzNizszN MkLjOUBl Ml7rbY5pcWKrdIOgNVTwxIViY3XscEBoem:5dHi= MWqyN|kyQDd7Nx?=
ZR-75-30 MlvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[zN{DPxE1? NFTyS2E2KGR? M1XuOolvcGmkaYTzJE0yPe,:hTDj[YxtKGe{b4f0bC=> NWeyS2xwOjN7MUi3PVc>

... 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
NCT02058381 Completed Pre-menopausal Breast Cancer|PI3K Pathway Inhibition Novartis Pharmaceuticals|Novartis May 6 2014 Phase 1
NCT02051751 Completed Neoplasms Breast Neoplasms Head and Neck Neoplasms Novartis Pharmaceuticals|Novartis March 5 2014 Phase 1
NCT01219699 Active not recruiting Advanced Solid Tumors With an Alteration of the PIK3CA Gene|Estrogen Receptor Positive Breast Cancer Novartis Pharmaceuticals|Novartis October 5 2010 Phase 1
NCT03601507 Not yet 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) September 30 2018 Phase 2
NCT02282371 Active not recruiting Head and Neck Squamous Cell Cancer Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals October 30 2014 Phase 1
NCT02155088 Active not recruiting Pancreatic Cancer H. Lee Moffitt Cancer Center and Research Institute|Novartis October 30 2014 Phase 1

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PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID