2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. Bimiralisib

Bimiralisib  (Synonyms: PQR309)

目录号: HY-12868 纯度: 99.80%
Data Sheet SDS COA 产品使用指南 技术支持

溶解度

动物溶解方案

Bimiralisib (PQR309) 是一种有效的，可渗透脑的，PI3K/mTOR 抑制剂，抑制 PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ 和 mTOR，IC50 分别为 33 nM，451 nM，661 nM，708 nM 和 89 nM。Bimiralisib 是 mTORC1 和 mTORC2 抑制剂。

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Bimiralisib Chemical Structure

Bimiralisib Chemical Structure

CAS No. : 1225037-39-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥946
In-stock
2 mg ￥500
In-stock
5 mg ￥860
In-stock
10 mg ￥1300
In-stock
25 mg ￥2620
In-stock
50 mg ￥4200
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Bimiralisib:

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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mTOR mTORC1 mTORC2

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.

IC50 & Target[1][2]

PI3Kα

33 nM (IC50)

PI3Kα-H1047R

36 nM (IC50)

PI3Kα-E542K

63 nM (IC50)

PI3Kα-E545K

136 nM (IC50)

PI3Kδ

451 nM (IC50)

PI3Kβ

661 nM (IC50)

PI3Kγ

708 nM (IC50)

Vps34

6486 nM (IC50)

mTOR

89 nM (IC50)

mTORC1

 

mTORC2

 

DNA-PK

8567 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2058 IC50
139 nM
Compound: 1; PQR309
Inhibition of mTORC2 in human A2058 cells assessed as reduction in PKB phosphorylation at S473 residues incubated for 1 hr by Western blot analysis
Inhibition of mTORC2 in human A2058 cells assessed as reduction in PKB phosphorylation at S473 residues incubated for 1 hr by Western blot analysis
[PMID: 31465220]
A2058 IC50
139 nM
Compound: 5; PQR309
Inhibition of Class 1 PI3K/mTOR in human A2058 cells assessed as reduction in Akt phosphorylation at Ser473 residue incubated for 1 hr by InCell Western assay
Inhibition of Class 1 PI3K/mTOR in human A2058 cells assessed as reduction in Akt phosphorylation at Ser473 residue incubated for 1 hr by InCell Western assay
[PMID: 31244112]
A2058 IC50
205 nM
Compound: 1; PQR309
Inhibition of mTORC1 in human A2058 cells assessed as reduction in ribosomal protein S6 phosphorylation at Ser235/236 residues incubated for 1 hr by Western blot analysis
Inhibition of mTORC1 in human A2058 cells assessed as reduction in ribosomal protein S6 phosphorylation at Ser235/236 residues incubated for 1 hr by Western blot analysis
[PMID: 31465220]
A2058 IC50
205 nM
Compound: 5; PQR309
Inhibition of Class 1 PI3K/mTOR in human A2058 cells assessed as reduction in S6 phosphorylation at Ser235/236 residue incubated for 1 hr by InCell Western assay
Inhibition of Class 1 PI3K/mTOR in human A2058 cells assessed as reduction in S6 phosphorylation at Ser235/236 residue incubated for 1 hr by InCell Western assay
[PMID: 31244112]
A2058 IC50
2333 nM
Compound: 1; PQR309
Antiproliferative activity against human A2058 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human A2058 cells after 48 hrs by sulforhodamine B assay
[PMID: 28829592]
SK-OV-3 IC50
237 nM
Compound: 1; PQR309
Antiproliferative activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay
[PMID: 28829592]
体外研究
(In Vitro)

Bimiralisib 是一种高度选择性的泛 PI3K 抑制剂，可平衡靶向 mTOR 激酶。Bimiralisib 还抑制 PI3Kα-H1047R、PI3Kα-E542K 和 PI3Kα-E545K，IC50 分别为 36 nM、63 nM 和 136 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

口服给药在大脑和血浆样本中产生相似浓度的 Bimiralisib，说明 Bimiralisib 很容易通过血脑屏障。在小鼠中，po 和 iv 应用途径均显示 PQR309 在给药后 <1 小时 (iv) 至 <2 小时 (po) 内迅速下降至 200 ng/mL (~0.5 μM) 以下，这反映了药物作用的时间点达到在肿瘤细胞系中测定的中值 GI50。在雌性大鼠中，就 Cmax 而言，单次口服剂量 (10 mg/kg) 达到与单次静脉注射 (5 mg/kg) 相似的药物水平。5-8 小时的半衰期和约 14 000 h?ng/mL 的 AUC0.25-12 促成了 PQR309 出色的口服生物利用度 (>50%)。口服给药后 24 小时，PQR309 的血浆水平仍然 > 2 μM (800-1000 ng/mL)。此外，在暴露于 PQR309 1-2 小时后，大鼠脑样本中的药物水平与血浆水平相当，证实 PQR309 快速进入大脑[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT03127020PIQUR Therapeutics AG|University Hospital, Basel, Switzerland|University Hospital Munich|University Hospital Freiburg|Charite University, Berlin, Germany|University of Stuttgart
Lymphoma|Non-Hodgkin Lymphoma
June 2016Phase 2
NCT01940133PIQUR Therapeutics AG
Advanced Solid Tumors
January 2014Phase 1
NCT02850744PIQUR Therapeutics AG|University Hospital, Basel, Switzerland|Insel Gruppe AG, University Hospital Bern|University Hospital, Zürich
Glioblastoma Multiforme
July 2015Phase 2
分子量

411.38

Formula

C17H20F3N7O2
CAS 号
性状

固体

颜色

White to gray

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 50 mg/mL (121.54 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4308 mL 12.1542 mL 24.3084 mL
5 mM 0.4862 mL 2.4308 mL 4.8617 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.08 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.08 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

扫码获得
动物溶解方案

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 网站选购。
纯度 & 产品资料
参考文献
Cell Assay
[1]

Human tumor cell lines are seeded into 96-well microtiter plates and exposed to five (1/2 log serial) drug dilutions plus control, followed by 48 h (except for two controls of each cell line which are fixed with TCA (cell population at t =0 h [Tz]). The assay is terminated by fixation with TCA (10% final). Cell density is determined using a sulforhodamine B staining protocol and the absorbance measured at 515 nm. Using seven absorbance measurements, the percentage growth is calculated at each of the drug concentrations levels. Percentage growth inhibition is calculated. The NTRC Oncolines 44 cell lines are exposed for 72 h to 9-point 3-fold serial dilutions of Bimiralisib. The concentration of 50% growth inhibition is associated with the signal ((luminescenceuntreated,t=72h-luminescencet=0)/2)+luminescencet=0. The data set integrated here is used for IC50 calculations. IC50 values of A2058 or SKOV3 cell proliferation given are determined and calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Healthy male nude NIH rats are used. 2×107 PC-3 cells are injected subcutaneously at day 0 (D0) in 200 μL of RPMI1640 into the right flank of male nude rats, 24 h after a whole-body irradiation with a γ-source (5 Gy, 60Co). Tumor-bearing rats are randomized on day 16 (mean volume of 330±70 mm3 according to their individual tumor volume into five groups of each eight animals using Vivo manager software. Analysis of variance is performed to test for homogeneity between groups. Daily administration on D17-D44 and from D51 to D57: group 1, vehicle; group 2, compound 1 at 5 mg/kg; group 3, Bimiralisib at 10 mg/kg. Group 4: Bimiralisib at 15 mg/kg from D17 to D21, from D24 to D28, from D34 to D38, from D41 to D4, and from D51 to D56. Group 5: one iv injection of Vinorelbine at 2.5 mg/kg on D17, D24, D31, and D38. Final termination of rats is performed on D87. Body weight is measured at least twice a week. Length and width of tumors are measured and recorded twice a week with calipers, and the tumor volume is estimated.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Bimiralisib 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4308 mL 12.1542 mL 24.3084 mL 60.7711 mL
5 mM 0.4862 mL 2.4308 mL 4.8617 mL 12.1542 mL
10 mM 0.2431 mL 1.2154 mL 2.4308 mL 6.0771 mL
15 mM 0.1621 mL 0.8103 mL 1.6206 mL 4.0514 mL
20 mM 0.1215 mL 0.6077 mL 1.2154 mL 3.0386 mL
25 mM 0.0972 mL 0.4862 mL 0.9723 mL 2.4308 mL
30 mM 0.0810 mL 0.4051 mL 0.8103 mL 2.0257 mL
40 mM 0.0608 mL 0.3039 mL 0.6077 mL 1.5193 mL
50 mM 0.0486 mL 0.2431 mL 0.4862 mL 1.2154 mL
60 mM 0.0405 mL 0.2026 mL 0.4051 mL 1.0129 mL
80 mM 0.0304 mL 0.1519 mL 0.3039 mL 0.7596 mL
100 mM 0.0243 mL 0.1215 mL 0.2431 mL 0.6077 mL

Keywords:

Bimiralisib1225037-39-7PQR309PQR 309PQR-309PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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