| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| 靶点 |
p110α (IC50 = 5 nM); p110γ (IC50 = 250 nM); p110δ (IC50 = 290 nM); p110β (IC50 = 1200 nM); p110α-H1047R (IC50 = 4 nM); p110α-E545K (IC50 = 4 nM)
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| 体外研究 (In Vitro) |
BYL719 抑制携带 PIK3CA 突变的乳腺癌细胞系的增殖，与抑制 PI3K/Akt 通路的各种下游信号成分相关。
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| 体内研究 (In Vivo) |
在啮齿类动物的 PIK3CA 突变异种移植模型中，BYL719（>270 mg/d）表现出统计学上显着的剂量依赖性抗肿瘤功效。 BYL719 的半衰期较短，为 8.5 小时，Cmax 个体间差异较低，在人体中暴露剂量在 30 mg/d 至 450 mg/d 之间按比例增加。 BYL719（270 mg/d）临床疗效的第一个迹象包括 1 名 ER+ 乳腺癌患者确认有部分缓解，在评估的 17 名患者中，有 8 名患者出现显着 PET 缓解 (PMR) 和/或肿瘤缩小。
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| 酶活实验 |
Alpelisib (NVP-BYL719) 有效抑制 2 种最常见的 PIK3CA 体细胞突变（H1047R、E545K；IC50~4 nM）。 Alpelisib (NVP-BYL719) 有效抑制 PI3Kα 转化细胞中的 Akt 磷酸化 (IC50=74±15 nM)，并在 PI3Kβ 或 PI3Kδ 异构体转化细胞中显示出显着降低的抑制活性（与 PI3Kα 相比≥15 倍）。
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| 细胞实验 |
Alpelisib (0–1000 nM) 以逐渐升高的浓度作用于细胞，持续 72 小时。使用 CyQuant 测定法测量细胞活力。
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| 动物实验 |
Female athymic nu/nu mice
40 mg/kg o.g. |
| 参考文献 |
| 分子式 |
C19H22F3N5O2S
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|---|---|
| 分子量 |
441.47
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| 精确质量 |
441.14463
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| 元素分析 |
C, 51.69; H, 5.02; F, 12.91; N, 15.86; O, 7.25; S, 7.26
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| CAS号 |
1217486-61-7
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| 相关CAS号 |
Alpelisib hydrochloride;1584128-91-5
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| 外观&性状 |
white solid powder
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| SMILES |
CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
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| InChi Key |
STUWGJZDJHPWGZ-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1
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| 化学名 |
(2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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| 别名 |
Alpelisib; NVP-BYL-719; NVP-BYL719; NVP-BYL 719; BYL-719; BYL719; BYL 719
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.33 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.71 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30mg/mL Solubility in Formulation 6: 10 mg/mL (22.65 mM) in 0.5% MC 0.5% Tween-80 (add these co-solvents sequentially from left to right, and one by one), Suspension solution; with ultrasonication. Solubility in Formulation 7: 10 mg/mL (22.65 mM) in 1% CMC 0.5% Tween-80 (add these co-solvents sequentially from left to right, and one by one), Suspension solution; with ultrasonication. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2652 mL | 11.3258 mL | 22.6516 mL | |
| 5 mM | 0.4530 mL | 2.2652 mL | 4.5303 mL | |
| 10 mM | 0.2265 mL | 1.1326 mL | 2.2652 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03056755 | Active Recruiting |
Drug: Alpelisib Drug: Fulvestrant |
Breast Cancer | Novartis Pharmaceuticals | August 14, 2017 | Phase 2 |
| NCT04729387 | Active Recruiting |
Drug: Alpelisib Drug: Olaparib |
Ovarian Cancer | Zenyaku Kogyo Co., Ltd. | July 2, 2021 | Phase 1 |
| NCT03439046 | Active Recruiting |
Drug: Alpelisib Drug: Ribociclib |
Breast Cancer | Novartis Pharmaceuticals | February 2, 2018 | Phase 3 |
| NCT04300790 | Active Recruiting |
Drug: Alpelisib Drug: Metformin |
Breast Cancer | MedSIR | October 23, 2020 | Phase 2 |
| NCT01872260 | Active Recruiting |
Drug: Alpelisib Drug: LEE011 |
Breast Cancer | Novartis Pharmaceuticals | October 22, 2013 | Phase 1 Phase 2 |
 PK/PD/efficacy relationship of NVP-BYL719 in PI3Kα-dependent tumor mouse modelsin vivo.Mol Cancer Ther.2014 May;13(5):1117-29. |
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 Determination of NVP-BYL719 safety profile compared with pan-class I PI3K inhibitors.Mol Cancer Ther.2014 May;13(5):1117-29. |
 PTENmutation andPIK3CAamplification/copy number modulate response to NVP-BYL719.Mol Cancer Ther.2014 May;13(5):1117-29. |
 A, genetic alterations inPIK3CApredict NVP-BYL719in vivoefficacy.B, PDX models carrying aPIK3CAmutation and/or amplification were established by implanting surgical tumor tissues from treatment-naïve cancer patients into athymic mice.Mol Cancer Ther.2014 May;13(5):1117-29. |
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PIK3CAmutation is the top positive predictor for NVP-BYL719 sensitivity. A, NVP-BYL719 sensitivity profile. Scatter plot showingAmax(%) by EC50values expressed in μmol/L of NVP-BYL719 in cell viability assays assessed on 474 cancer cell lines.Mol Cancer Ther.2014 May;13(5):1117-29. |
 Identification of selectivity index of small molecule inhibitors forPIK3CAmutant versusPIK3CAwild-type (WT) cell line populations across ∼1,000 different compounds.Mol Cancer Ther.2014 May;13(5):1117-29. |
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