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Alpelisib (BYL719)
中文名稱：阿培利司
Alpelisib (BYL719) 是一種有效的選擇性PI3Kα抑制劑，在無細胞試驗中IC50為 5 nM，對PI3Kβ/γ/δ具有極弱的作用。Phase 2。
Alpelisib (BYL719) Chemical Structure
CAS: 1217486-61-7
產(chǎn)品質(zhì)控
批次：
純度：
99.96%
99.96
Alpelisib (BYL719)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| H929 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| MM1S | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| MM1R | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| U266 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| OPM1 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| OPM2 | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| Mel290 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| C918 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| Omm1 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| Omm1.3 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| Mel270 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| 92.1 | Growth Inhibition Assay | 500-2000 nM | 5 d | inhibits the phosphorylation of AKT (Ser473) up to 1 μM | 24563540 |
| QGP-1 | Function Assay | 1/10 μM | 4 h | inhibits PI3K (AKT Ser308) and mTORC1/2 activities | 25026292 |
| BON-1 | Function Assay | 1/10 μM | 4 h | inhibits PI3K (AKT Ser308) and mTORC1/2 activities | 25026292 |
| SCC25 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=49.30 μM | 25550549 |
| SNU1041 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=20.65 μM | 25550549 |
| FaDu | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=19.66 μM | 25550549 |
| SNU-1066 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=1.13 μM | 25550549 |
| SNU-1076 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=6.82 μM | 25550549 |
| Detroit562 | Growth Inhibition Assay | 0.1-100 μM | 72 h | IC50=1.10 μM | 25550549 |
| RPMI | Growth Inhibition Assay | 0.5-2.5 μM | 48 h | inhibits cell growth in a dose-dependent manner | 24405121 |
| SKBR3 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 35％ cell growth | 23918797 |
| MDA453 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 38％ cell growth | 23918797 |
| EFM192A | Growth Inhibition Assay | 33 μM | 5 d | inhibits 27％ cell growth | 23918797 |
| AU565 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 26％ cell growth | 23918797 |
| MDA361 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 44％ cell growth | 23918797 |
| BT474 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 16％ cell growth | 23918797 |
| HCC202 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 20％ cell growth | 23918797 |
| KPL4 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 58％ cell growth | 23918797 |
| NCL-N87 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 31％ cell growth | 23918797 |
| UACC812 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 27％ cell growth | 23918797 |
| HCC2218 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 15％ cell growth | 23918797 |
| HCC1569 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 5％ cell growth | 23918797 |
| OE19 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 23％ cell growth | 23918797 |
| OE33 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 23％ cell growth | 23918797 |
| JIMT1 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 9％ cell growth | 23918797 |
| HCC1954 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 29％ cell growth | 23918797 |
| NUGC4 | Growth Inhibition Assay | 33 μM | 5 d | inhibits 14％ cell growth | 23918797 |
| ZR-75-30 | Growth Inhibition Assay | 33 μM | 5 d | inhibits -15％ cell growth | 23918797 |
| POS-1 | Growth Inhibition Assay | IC50=8 μM， IC90=36 μM | 24961790 | ||
| MOS-J | Growth Inhibition Assay | IC50=10 μM， IC90=36 μM | 24961790 | ||
| HOS | Growth Inhibition Assay | IC50=15 μM， IC90=42 μM | 24961790 | ||
| MG-63 | Growth Inhibition Assay | IC50=6 μM， IC90=24 μM | 24961790 | ||
| Rat1 | P110alpha inhibition assay | IC50 = 0.074 μM | 26164189 | ||
| Rat1 | PI3Kalpha inhibition assay | IC50 = 0.074 μM | 26206504 | ||
| Rat1 | P110alpha inhibition assay | IC50 = 0.074 μM | 23726034 | ||
| Rat1 | P110delta inhibition assay | IC50 = 1.2 μM | 26164189 | ||
| Rat1 | PI3Kgamma inhibition assay | IC50 = 1.2 μM | 26206504 | ||
| Rat1 | P110delta inhibition assay | IC50 = 1.2 μM | 23726034 | ||
| Rat1 | P110beta inhibition assay | IC50 = 2.2 μM | 26164189 | ||
| Rat1 | PI3Kbeta inhibition assay | IC50 = 2.2 μM | 26206504 | ||
| Rat1 | P110alpha inhibition assay | IC50 = 2.2 μM | 23726034 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Alpelisib (BYL719) 是一種有效的選擇性PI3Kα抑制劑，在無細胞試驗中IC50為 5 nM，對PI3Kβ/γ/δ具有極弱的作用。Phase 2。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | BYL719抑制含有PIK3CA突變體的乳腺癌細胞系的增殖，與PI3K/Akt通路各種下游信號組分的抑制相關(guān)。[1] |
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-AKT(S473) / p-AKT(T308) p100β / p110α / p85 / p-ERBB3(Y1289) p-HER2 / IGF-1R pS6 (Ser235-236) PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD |
|
25544637 | |
| Growth inhibition assay | Cell viability |
|
27602501 | |
| Immunofluorescence | LC3 |
|
26637440 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | BYL719(>270 mg/d)在PIK3CA突變體異種移植嚙齒動物模型中表現(xiàn)出統(tǒng)計學(xué)顯著的劑量依賴性抗腫瘤效能。BYL719具有低清除率，半衰期為8.5小時，并且它的作用在30mg/d 和450mg/d之間劑量成比例的增加，在人的Cmax 和AUC中顯示出低的個體差異。BYL719(270mg/d)首次表現(xiàn)出臨床療效的跡象，包括在ER+乳腺癌患者中證實的部分響應(yīng)，以及17個患者中8個實現(xiàn)了顯著的PET響應(yīng)(PMR)和/或腫瘤治愈。[1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05948943 | Recruiting | Lymphatic Malformations |
Novartis Pharmaceuticals|Novartis |
November 24 2023 | Phase 2|Phase 3 |
| NCT05660083 | Recruiting | HER2-negative Breast Cancer|Metastatic Breast Cancer|Metaplastic Breast Carcinoma|TNBC - Triple-Negative Breast Cancer |
The Methodist Hospital Research Institute|Novartis Pharmaceuticals |
January 12 2023 | Phase 2 |
| NCT05508906 | Recruiting | Metastatic Breast Cancer|Advanced Breast Cancer|HR-positive Breast Cancer|HER2-negative Breast Cancer |
Olema Pharmaceuticals Inc.|Novartis |
August 31 2022 | Phase 1 |
| NCT05230810 | Recruiting | HER2-positive Metastatic Breast Cancer |
Criterium Inc.|Novartis|Seagen Inc. |
August 25 2022 | Phase 1|Phase 2 |
化學(xué)信息&溶解度
| 分子量 | 441.47 | 分子式 | C19H22F3N5O2S |
| CAS號 | 1217486-61-7 | SDF | Download Alpelisib (BYL719) SDF |
| Smiles | CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 88 mg/mL ( (199.33 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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