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Buparlisib (BKM120, NVP-BKM120)

别名: Buparlisib; BKM120; BKM-120; BKM 120; NVPBKM120; NVP BKM120; BKM120; NVP-BKM120; 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine; BKM-120; NVP-BKM-120; 1202777-78-3; NV-BKM120 布帕利司；5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺; 5-（2,6-二吗啉基嘧啶-4-基）-4-（三氟甲基）吡啶-2-胺; 5-[2,6-二(4-吗啉)-4-嘧啶]-4-(三氟甲基)-2-吡啶胺; BKM120 (NVP-BKM120, Buparlisib) ;BKM120粉末;BKM120中间体;NVP-BKM120靶向药;NVP-BKM120固体状;科研实验NVP-BKM120;临床实验NVP-BKM120;医药级BKM120;BKM120;布帕尼西
目录号: V0105 纯度: ≥98%
COA 产品数据 产品说明书 SDS
BKM120（也称为 NVP-BKM120 或 Buparlisib）是一种选择性、口服生物利用度和有效的 p110α/β/δ/γ 泛 I 类 PI3K 抑制剂，在无细胞测定中的 IC50 为 52 nM/166 nM/116 nM/262 nM 。
Buparlisib (BKM120, NVP-BKM120) CAS号: 944396-07-0
产品类别: PI3K
产品仅用于科学研究，不针对患者销售
规格 价格 库存 数量
10 mM * 1 mL in DMSO
1mg
5mg
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes
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Other Forms of Buparlisib (BKM120, NVP-BKM120):

  • 盐酸布帕尼西
点击了解更多
InvivoChem产品被CNS等顶刊论文引用
纯度/质量控制文件

纯度: ≥98%

纯度: ≥98%

COA
MSDS
NMR
HPLC
COA
MSDS
NMR
产品说明书
产品描述
BKM120（也称为 NVP-BKM120 或 Buparlisib）是一种选择性的、口服生物可利用的、有效的 p110α/β/δ/γ 泛 I 类 PI3K 抑制剂，在无细胞测定中的 IC50 为 52 nM/166 nM/116 nM/262 nM 。它具有抗癌活性。它对 VPS34、mTOR、DNAPK 的有效性减弱，对 PI4K 几乎没有活性。已经开展了多项涉及 BKM120 治疗各种癌症的临床试验。细胞增殖、生长、存活、凋亡、蛋白质合成和葡萄糖代谢等细胞过程受细胞内磷脂酰肌醇 3 激酶 (PI3K) 途径的调节。 2-吗啉代嘧啶衍生物的生物学特征 BKM120 是一种泛 PI3K 抑制剂。根据体外研究，NVP-BKM120 在生化测定中抑制所有四种 I 类 PI3K 亚型，选择性比其他蛋白激酶至少高 50 倍。
生物活性&实验参考方法
靶点
p110α (IC50 = 52 nM); p110β (IC50 = 166 nM); p110δ (IC50 = 116 nM); p110γ (IC50 = 262 nM); Vps34 (IC50 = 2.4 μM); p110α-H1047R (IC50 = 52 nM); p110α-E545K (IC50 = 99 nM); mTOR (IC50 = 4.6 μM)
体外研究 (In Vitro)
Buparlisib (NVP-BKM120) 对 I 类 PI3K（包括最常见的 p110α 突变体）表现出 50-300 nM 的活性。此外，NVP-BKM120 对 III 类和 IV 类 PI3K 的效果较差，分别在 2、5、>5 和 >25 μM 时检测到抑制 VPS34、mTOR、DNAPK 和 PI4K 的生化活性[1] 。 Buparlisib (NVP-BKM120) 诱导多发性骨髓瘤 (MM) 细胞凋亡，其方式取决于剂量和时间的推移。在浓度 ≥10 μM 时，buparlisib (NVP-BKM120) 在 24 小时内显着诱导所有测试的 MM 细胞系凋亡（与对照相比，P<0.05）。如果没有另外说明，以下实验将使用 ≥10 μM buparlisib (NVP-BKM120) 和 24 小时治疗周期。所有测试的 MM 细胞系均表现出对 buparlisib (NVP-BKM120) 治疗的剂量依赖性生长抑制。 Buparlisib (NVP-BKM120) IC50 在测试的 MM 细胞之间存在差异。处理 24 小时时，ARP-1、ARK 和 MM.1R 的 IC50 为 1 至 <10 μM，而 MM.1S 的 IC50 小于 <1 μM，U266 的 IC50 为 10 至 <10 μM。 <100μM，。总之，NVP-BKM120 治疗可抑制 MM 细胞的生长并导致其死亡，具体方式取决于剂量和时间长度[2]。
体内研究 (In Vivo)
在 A2780 异种移植肿瘤中，口服 3、10、30、60 和 100 mg/kg 剂量的 Buparlisib (NVP-BKM120) 会导致 pAKTSer473 的剂量依赖性调节。在3和10mg/kg的剂量下，观察到pAKTSer473的部分抑制，在30、60或100mg/kg的剂量下，观察到几乎完全的抑制。血浆和肿瘤药物暴露均与 pAKT 抑制（标准化为总 AKT）密切相关[1]。 Buparlisib (NVP-BKM120)（5 M/kg/天，持续 15 天）治疗小鼠的肿瘤负荷显着低于对照小鼠，如肿瘤体积 (P<0.05) 和循环人 kappa 链水平 (P<0.05) 所示。此外，NVP-BKM120治疗显着提高了荷瘤小鼠的存活率（P<0.05）[2]。
酶活实验
BKM120 溶解在 DMSO 中，并以每孔 1.25 µL 的量直接分配到黑色 384 孔板中。要开始反应，请在测定缓冲液（10 mM Tris pH 7.5、5 mM MgCl2、20 mM NaCl、1 mM DTT 和 0.05% CHAPS）中添加 25 µL 10 nM PI3 激酶和 5 µg/mL 1-磷脂酰肌醇 (PI) ）进入每个井。接下来，在测定缓冲液中添加 25 L 2 M ATP。在反应运行到耗尽 ATP 所需时间的大约 50% 后，添加 25 L KinaseGlo 溶液会停止反应。孵育 5 分钟后，检查停止的反应以确定是否仍然存在任何 ATP。
细胞实验
A2780 细胞在补充有 10% FBS 的 DMEM 中培养。 L-谷氨酰胺、丙酮酸钠和抗生素。在黑壁透明底板中，将 1000 个细胞以每孔 100 uL 的密度接种在相同的培养基中，然后将细胞孵育 3 至 5 小时。将在 DMSO (20 mM) 中提供的 Buparlisib (NVP-BKM120) 在 DMSO 中进一步稀释（7.5 uL 20 mM Buparlisib 在 22.5 uL DMSO 中）。为了制备九个浓度，重复充分混合并添加 10 uL 至 20 uL DMSO 的过程。然后将稀释的 Buparlisib (NVP-BKM120) 溶液 (2 uL) 添加到细胞培养基 (500 uL) 中。将等量的该溶液 (100 uL) 倒在 96 孔板中的细胞顶部，然后在 37°C 下孵育三天，然后使用 Cell Titer Glo 进行显色。 Trilux 的发光读数用于确定细胞增殖是否受到抑制[1]。
动物实验
Mice: The SCID (severe combined immunodeficiency) mouse model is a female, six to eight week old mouse. One million ARP-1 or MM.1S cells suspended in 50 μL phosphate-buffered saline (PBS) are subcutaneously injected into SCID mice in the right flank. DMSO/PBS or Buparlisib (NVP-BKM120) (5 μM per kg per day) are administered intraperitoneally to mice 15 days after the development of a palpable tumor (tumor diameter ≥5 mm). Each time a blood sample is taken, tumor sizes are also measured every five days. The size of the tumor and the presence of human kappa chain or lambda chain in the bloodstream are used to assess the burden of the tumor.
参考文献

[1]. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer. ACS Med Chem Lett. 2011 Aug 26;2(10):774-9.

[2]. Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity. J Mol Med (Berl). 2012 Jun;90(6):695-706.

[3]. Combination inhibition of PI3K and mTORC1 yields durable remissions in mice bearing orthotopic patient-derived xenografts of HER2-positive breast cancer brain metastases. Nat Med. 2016 Jul;22(7):723-6.

[4]. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369.
其他信息
BKM120 is an aminopyridine that is 4-(trifluoromethyl)pyridin-2-amine substituted at position 5 by a 2,6-di(morpholin-4-yl)pyrimidin-4-y group. A selective PI3K inhibitor with anti-tumour properties. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an antineoplastic agent. It is a member of morpholines, an aminopyrimidine, an aminopyridine and an organofluorine compound.
Buparlisib has been used in trials studying the treatment and basic science of Lymphoma, Metastases, Lung Cancer, Solid Tumors, and Breast Cancer, among others.
Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. Buparlisib specifically inhibits class I PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C18H21F3N6O2
分子量
410.3936
精确质量
410.167
元素分析
C, 52.68; H, 5.16; F, 13.89; N, 20.48; O, 7.80
CAS号
944396-07-0
相关CAS号
Buparlisib Hydrochloride;1312445-63-8
PubChem CID
16654980
外观&性状
white solid powder
密度
1.4±0.1 g/cm3
沸点
645.7±65.0 °C at 760 mmHg
闪点
344.3±34.3 °C
蒸汽压
0.0±1.9 mmHg at 25°C
折射率
1.574
LogP
2.08
tPSA
89.63
氢键供体(HBD)数目
1
氢键受体(HBA)数目
11
可旋转键数目(RBC)
3
重原子数目
29
分子复杂度/Complexity
530
定义原子立体中心数目
0
SMILES
FC(C1C(C2C=C(N3CCOCC3)N=C(N3CCOCC3)N=2)=CN=C(N)C=1)(F)F
InChi Key
CWHUFRVAEUJCEF-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H21F3N6O2/c19-18(20,21)13-9-15(22)23-11-12(13)14-10-16(26-1-5-28-6-2-26)25-17(24-14)27-3-7-29-8-4-27/h9-11H,1-8H2,(H2,22,23)
化学名
5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine.
别名
Buparlisib; BKM120; BKM-120; BKM 120; NVPBKM120; NVP BKM120; BKM120; NVP-BKM120; 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine; BKM-120; NVP-BKM-120; 1202777-78-3; NV-BKM120
HS Tariff Code
2934.99.9001
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)
溶解度数据
溶解度 (体外实验)
DMSO: ~82 mg/mL (199.8 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 2 mg/mL (4.87 mM)
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 2.5 mg/mL (6.09 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。
配方 2 中的溶解度: ≥ 2.5 mg/mL (6.09 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。
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配方 3 中的溶解度: ≥ 2.5 mg/mL (6.09 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

配方 4 中的溶解度: ≥ 2.5 mg/mL (6.09 mM) (饱和度未知) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。
配方 5 中的溶解度: ≥ 2.5 mg/mL (6.09 mM) (饱和度未知) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。
配方 6 中的溶解度: 0.5%CMC Na:6mg/mL
配方 7 中的溶解度: 2.08 mg/mL (5.07 mM) in 50% PEG300 50% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浊液; 超声助溶。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
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 2.4367 mL 12.1835 mL 24.3671 mL
5 mM 0.4873 mL 2.4367 mL 4.8734 mL
10 mM 0.2437 mL 1.2184 mL 2.4367 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。

计算器
计算 重置

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度，具体如下：

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示：
假如化合物的分子量为350.26 g/mol，在5mL DMSO中制备10mM储备液所需的化合物的质量是多少？
  • 在分子量（MW）框中输入350.26
  • 在“浓度”框中输入10，然后选择正确的单位（mM）
  • 在“体积”框中输入5，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式，您可以计算体积和浓度。
计算 重置

稀释计算器可计算如何稀释已知浓度的储备液。例如，可以输入C1、C2和V2来计算V1，具体如下：

制备25毫升25μM溶液需要多少体积的10 mM储备溶液？
使用方程式C1V1=C2V2，其中C1=10mM，C2=25μM，V2=25 ml，V1未知：
  • 在C1框中输入10，然后选择正确的单位（mM）
  • 在C2框中输入25，然后选择正确的单位（μM）
  • 在V2框中输入25，然后选择正确的单位（mL）
  • 单击“计算”按钮
  • 答案62.5μL（0.1 ml）出现在V1框中
g/mol
计算 重置

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成，具体如下：

注：化学分子式大小写敏感：C12H18N3O4  c12h18n3o4
计算化合物摩尔质量（分子量）的说明：
  • 要计算化合物的分子量 (摩尔质量)，请输入化学/分子式，然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义：
  • 分子质量（或分子量）是一种物质的一个分子的质量，用统一的原子质量单位（u）表示。（1u等于碳-12中一个原子质量的1/12）
  • 摩尔质量（摩尔重量）是一摩尔物质的质量，以g/mol表示。
/
计算 重置

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶/难溶于水的化合物），不同的产品和批次配方组成不同，如对配方有疑问，可先联系我们提供正确的体内实验配方。此外，请注意这只是一个配方计算器，而不是特定产品的确切配方。
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+
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计算 重置

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) 。

临床试验信息
Phase Ib Study of BKM120 With Cisplatin and XRT in High Risk Locally Advanced Squamous Cell Cancer of Head and Neck
CTID: NCT02113878
Phase: Phase 1    Status: Completed
Date: 2024-11-05
LGX818 and MEK162 in Combination With a Third Agent (BKM120, LEE011, BGJ398 or INC280) in Advanced BRAF Melanoma
CTID: NCT02159066
Phase: Phase 2    Status: Completed
Date: 2024-03-05
GINECO-EN102b - BKM120 as Monotherapy in the Treatment of Initial or Recurrent Metastatic Endometrial Cancer
CTID: NCT01397877
Phase: Phase 2    Status: Completed
Date: 2023-09-06
Buparlisib in Patients With Relapsed and Refractory Chronic Lymphocytic Leukemia
CTID: NCT02340780
Phase: Phase 2    Status: Completed
Date: 2023-08-22
P13Kinase Inhibitor BKM120 in Combination With Panitumumab in Metastatic/Advanced RAS-Wild Type Colorectal Cancer.
CTID: NCT01591421
Phase: Phase 1/Phase 2    Status: Completed
Date: 2023-08-04
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Buparlisib, Gemcitabine Hydrochloride, and Cisplatin in Treating Patients With Advanced Solid Tumors
CTID: NCT01971489
Phase: Phase 1    Status: Withdrawn
Date: 2023-04-27

A Clinical Trial of Buparlisib and Ibrutinib in Lymphoma
CTID: NCT02756247
Phase: Phase 1    Status: Completed
Date: 2022-10-10
Phase I BKM120/Abraxane in Solid Tumors, Expansion Phase Recurrent Endometrial or Ovarian Cancer
CTID: NCT02117817
Phase: Phase 1    Status: Withdrawn
Date: 2022-07-28
A Study of BKM120 (Buparlisib) in Relapsed or Refractory Thymomas
CTID: NCT02220855
Phase: Phase 2    Status: Completed
Date: 2022-04-11
STAR Cape+BKM120 MBC With Brain Met
CTID: NCT02000882
Phase: Phase 2    Status: Completed
Date: 2022-02-07
BKM120 in Esophageal Squamous Cell Carcinoma After Failure of First Line Chemotherapy
CTID: NCT01806649
Phase: Phase 2    Status: Terminated
Date: 2021-10-11
Buparlisib in Metastatic Transitional Cell Carcinoma of the Urothelium
CTID: NCT01551030
Phase: Phase 2    Status: Completed
Date: 2021-06-21
Neoadjuvant BKM120 in High-risk Prostate Cancer
CTID: NCT01695473
Phase: Phase 2    Status: Terminated
Date: 2021-01-13
A Dose-finding Study of a Combination of Imatinib and BKM120 in the Treatment of 3rd Line GIST Patients
CTID: NCT01468688
Phase: Phase 1    Status: Completed
Date: 2020-12-21
Dose Escalation Study of LEE011 in Combination With Buparlisib and Letrozole in HR+, HER2-negative Post-menopausal Women With Advanced Breast Cancer.
CTID: NCT02154776
Phase: Phase 1    Status: Completed
Date: 2020-12-19
Phase Ib, Dose Escalation Study of Oral LDE225 in Combination With BKM120 in Patients With Advanced Solid Tumors
CTID: NCT01576666
Phase: Phase 1    Status: Completed
Date: 2020-12-19
A Study to Find the Maximum Tolerated Dose of the Experimental Combination of the Drugs INC424 and BKM120 in Patients With Primary or Secondary Myelofibrosis
CTID: NCT01730248
Phase: Phase 1    Status: Terminated
Date: 2020-12-19
Study of LEE011 With Fulvestrant and BYL719 or BKM120 in Advanced Breast Cancer
CTID: NCT02088684
Phase: Phase 1    Status: Completed
Date: 2020-12-17
A Phase I Dose Escalation Study of BKM120 With Radiation Therapy and Temozolomide in Patients With Newly Diagnosed Glioblastoma
CTID: NCT01473901
Phase: Phase 1    Status: Completed
Date: 2020-12-09
A Trial of Oral BEZ235 and BKM120 in Combination With Paclitaxel With or Without Trastuzumab
CTID: NCT01285466
Phase: Phase 1    Status: Completed
Date: 2020-12-09
A Phase I Study of BKM120 in Adult Chinese Patients With Advanced Solid Tumors
CTID: NCT01626209
Phase: Phase 1    Status: Completed
Date: 2020-12-09
Pharmacokinetic Study of BKM120 in Subjects With Hepatic Impairment
CTID: NCT01727128
Phase: Phase 1    Status: Completed
Date: 2020-12-09
Phase Ib/II Study of Buparlisib Plus Carboplatin or Lomustine in Patients With Recurrent Glioblastoma Multiforme
CTID: NCT01934361
Phase: Phase 1    Status: Completed
Date: 2020-12-09
Pharmacokinetic Study of Buparlisib in Subjects With Renal Impairment.
CTID: NCT02048787
Phase: Phase 1    Status: Completed
Date: 2020-12-09
Phase Ib of Abiraterone Acetate Plus BEZ235 or BKM120 in Castration-resistant Prostate Cancer (CRPC) Patients
CTID: NCT01634061
Phase: Phase 1    Status: Completed
Date: 2020-12-09
A Study to Investigate Safety, Pharmacokinetics (PK) and Pharmacodynamics (PD) of BKM120 Plus GSK1120212 in Selected Advanced Solid Tumor Patients
CTID: NCT01155453
Phase: Phase 1    Status: Completed
Date: 2020-12-09
A Study of BKM120 in Adult Japanese Patients With Advanced Solid Tumors
CTID: NCT01283503
Phase: Phase 1    Status: Completed
Date: 2020-12-08
Safety of BKM120 Monotherapy in Advanced Solid Tumor Patients
CTID: NCT01068483
Phase: Phase 1    Status: Completed
Date: 2020-12-08
A Trial of BKM120 (a PI3K Inhibitor) in Patients With Triple Negative Metastatic Breast Cancer
CTID: NCT01629615
Phase: Phase 2    Status: Completed
Date: 2020-10-28
Safety, Pharmacokinetics and Pharmacodynamics of BKM120 Plus MEK162 in Selected Advanced Solid Tumor Patients
CTID: NCT01363232
Phase: Phase 1    Status: Completed
Date: 2020-10-05
Phase III Study of BKM120/Placebo With Fulvestrant in Postmenopausal Patients With Hormone Receptor Positive HER2-negative Locally Advanced or Metastatic Breast Cancer Refractory to Aromatase Inhibitor
CTID: NCT01610284
Phase: Phase 3    Status: Completed
Date: 2020-08-25
Combination of BKM120 and Bevacizumab in
A Phase Ib/II, open-label, multicenter study of INC280 in combination with buparlisib in adult patients with recurrent glioblastoma
CTID: null
Phase: Phase 1, Phase 2    Status: Completed, Prematurely Ended
Date: 2014-02-26
Phase Ib/II multicenter study of buparlisib plus carboplatin or lomustine in patients with recurrent glioblastoma multiforme (GBM)
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2014-02-25
A phase II randomized, double-blind placebo controlled, study of letrozole with or without BYL719 or buparlisib, for the neoadjuvant treatment of postmenopausal women with hormone receptor-positive HER2-negative breast cancer.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-11-26
Phase II, Multi-center, Open-label Study of Single-agent LGX818 Followed by a Rational Combination With Agents After Progression on LGX818, in Adult Patients With Locally Advanced or Metastatic BRAF V600 Melanoma
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2013-10-12
Phase II multicenter randomized, double blind, placebo controlled study assessing the efficacy of buparlisib (BKM120) plus paclitaxel vs. placebo plus paclitaxel in patients with platinum pre-treated recurrent or metastatic head and neck squamous cell carcinoma.
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2013-08-28
A Phase Ib/II study of docetaxel with or without buparlisib as second line therapy for patients with advanced or metastatic squamous non-small cell lung cancer
CTID: null
Phase: Phase 1, Phase 2    Status: Completed, Prematurely Ended
Date: 2013-07-11
NeoPHOEBE: Pi3k inhibition in Her2 OverExpressing Breast cancEr
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-07-05
A dose-finding phase Ib study followed by a randomized, double-blind phase II study of carboplatin and paclitaxel with or without buparlisib in patients with previously untreated metastatic non-small cell lung cancer (NSCLC) of squamous histology
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2013-06-20
A phase Ib/II open-label study evaluating safety and efficacy of oral BKM120 in combination with lapatinib in HER2+/PI3K-activated, trastuzumab-resistant locally advanced, recurrent and metastatic breast cancer.
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2013-06-12
Phase 2 multicenter study to assess the safety and efficacy of BKM120 as monotherapy in the treatment of initial or recurrent metastatic endometrial cancer after first line therapy in patients who cannot undergo local surgery and/or radiotherapy.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-06-11
An open-label phase II study of BKM120 in patients with relapsed and refractory diffuse large B-cell lymphoma, mantle cell lymphoma and follicular lymphoma
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-03-07
A multicenter phase II pilot open label study to evaluate the efficacy and safety of BKM120 in the treatment of patients with advanced or metastatic differentiated thyroid cancers
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-03-06
PIK-ORL: A Phase II, multicenter trial aiming to evaluate BKM120 in monotherapy in patients with metastatic head and neck cancer recurrent or progressive under platin and cetuximab-based chemotherapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-01-17
Phase Ib dose finding study of abiraterone acetate plus BEZ235 or BKM120 in patients with castration-resistant prostate cancer
CTID: null
Phase: Phase 2    Status: Temporarily Halted
Date: 2012-10-17
A phase III randomized, double-blind placebo controlled study of BKM120 with fulvestrant, in postmenopausal women with hormone receptor-positive HER2-negative locally advanced or metastatic breast cancer which progressed on or after aromatase inhibitor treatment.
CTID: null
Phase: Phase 3    Status: Completed, Prematurely Ended
Date: 2012-09-13
A phase III randomized, double blind, placebo controlled study of BKM120 with fulvestrant, in postmenopausal women with hormone receptor-positive HER2-negative AI treated, locally advanced or metastatic breast cancer who progressed on or after mTOR inhibitor based treatmen
CTID: null
Phase: Phase 3    Status: Completed, Temporarily Halted, Prematurely Ended
Date: 2012-08-10
A randomized, double-blind, placebo controlled, phase II/III study of BKM120 plus paclitaxel in patients with HER2 negative inoperable locally advanced or metastatic breast cancer, with or without PI3K pathway activation.
CTID: null
Phase: Phase 2, Phase 3    Status: Temporarily Halted, Completed
Date: 2012-07-24
A phase II trial of BKM120 (a PI3K inhibitor) in patients with triple negative metastatic breast cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-03-20
An open label two-stage study of orally administered BKM120 in patients with metastatic non-small cell lung cancer with activated PI3K pathway
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-06-22
Estudio de fase II, de una sola rama, de BKM120 administrado por vía oral como tratamiento de segunda línea en pacientes con carcinoma endometrial avanzado
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2011-04-26
A Phase Ib/II, open label, multi-center study evaluating the safety and efficacy of BKM120 in combination with trastuzumab in patients with relapsing HER2 overexpressing breast cancer who have previously failed trastuzumab
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2011-01-17

生物数据图片

  • BKM120 (NVP-BKM120, Buparlisib)

    Analysis ofbuparlisibsubstrate affinity for ABC transporters usingin vitrotransport assays.2018 Jul 17;8(1):10784.

  • BKM120 (NVP-BKM120, Buparlisib)

    Theimpact of P-gp and BCRP on the brain and tissue penetration of buparlisib.


    BKM120 (NVP-BKM120, Buparlisib)

    Buparlisibhas excellent intracranial target engagement and oral bioavailability.2018 Jul 17;8(1):10784.

  • BKM120 (NVP-BKM120, Buparlisib)


    BKM120 (NVP-BKM120, Buparlisib)

    NVP-BKM120inhibits cancer cell proliferation and induces apoptosis in a CCA mouse model.2018 Aug;16(2):1627-1633.

  • BKM120 (NVP-BKM120, Buparlisib)

    Growth inhibition effect ofNVP-BKM120on CCA cell lines.2018 Aug;16(2):1627-1633.


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