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

Pilaralisib  (Synonyms: XL-147; SAR245408)

目录号: HY-16526 纯度: 99.69%
COA 产品使用指南

摩尔计算器

Pilaralisib (XL147; SAR245408) 是一种有效的选择性 I 类 PI3Ks 抑制剂，抑制 PI3Kα，PI3Kβ，PI3Kγ 和 PI3Kδ，IC50 分别为 39 nM，383 nM，23 nM 和 36 nM。

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Pilaralisib Chemical Structure

Pilaralisib Chemical Structure

CAS No. : 934526-89-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥893
In-stock
5 mg ￥750
In-stock
10 mg ￥1200
In-stock
50 mg ￥3000
In-stock
100 mg ￥4800
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Pilaralisib 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

IC50 & Target

PI3Kα

39 nM (IC50)

PI3Kβ

383 nM (IC50)

PI3Kδ

36 nM (IC50)

PI3Kγ

23 nM (IC50)

Vps34

6974 nM (IC50)

DNA-PK

4750 nM (IC50)

体外研究
(In Vitro)

Pilaralisib (XL147) displays potent inhibitory activity against Class I PI3K isoforms p110α, p110δ, and p110γ, with IC50s of 39, 36, and 23 nM, respectively. Pilaralisib (XL147) is less potent against the remaining Class I isoform, p110β, with an IC50 value of 383 nM. The IC50 value for inhibition of PI3Kα by Pilaralisib (XL147) is determined at various concentrations of ATP, revealing XL147 to be an ATP-competitive inhibitor with an equilibrium inhibition constant (Ki) value of 42 nM. Pilaralisib (XL147) has relatively weak inhibitory activity toward the class III PI3K vacuolar sorting protein 34 (VPS34; IC50 value of ~7.0 M) and the PI3K-related DNA-dependent protein kinase (DNA-PK; IC50 value of 4.75 μM). In an mTOR kinase immunoprecipitation assay using cell lysates, Pilaralisib (XL147) does not inhibit mTOR activity toward the physiologic substrate protein eukaryotic translation initiation factor 4E-binding protein 1 (4EBP1; IC50>15 μM). Consistent with its inhibitory activity against purified PI3K proteins, Pilaralisib (XL147) inhibits EGF-induced PIP3 production in PC-3 and MCF7 cells in serum-free medium with IC50s of 220 and 347 nM, respectively. The ability of Pilaralisib (XL147) to inhibit phosphorylation of key signaling proteins downstream of PI3K is examined by assessing its effects on EGF-stimulated phosphorylation of AKT and on nonstimulated phosphorylation of S6 in PC-3 cells in serum-free media by cell-based ELISA. Pilaralisib (XL147) inhibits these activities with IC50s of 477 and 776 nM, respectively[1].

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

Pilaralisib 相关抗体:
体内研究
(In Vivo)

The ability of Pilaralisib (XL147) to inhibit this endogenous phosphorylation of AKT, p70S6K, and S6 is examined following a single oral dose of 10, 30, 100, or 300 mg/kg. The tumors are harvested 4, 24, or 48 hours postdose and homogenized in lysis buffer. Tumor lysates from each animal (n=4) are then pooled for each group and analyzed for levels of total and phosphorylated AKT, p70S6K, and S6 by Western immunoblotting. Administration of Pilaralisib (XL147) causes a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4 hours. The dose-response relationships derived from the 4-hour time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation at doses of approximately 100 mg/kg (pAKTT308), 54 mg/kg (pAKTS473), 71 mg/kg (p-p70S6K), and 103 mg/kg (pS6). The inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 100 mg/kg dose of Pilaralisib (XL147) is maximal at 4 hours, reaching 55% to 75%; however, the level of inhibition decreased to 8% to 45% by 24 hours, and only minimal or no inhibition was evident by 48 hours. Following a 300 mg/kg dose of Pilaralisib (XL147), inhibition is also maximal at 4 hours (65%-81%). However, in contrast with the 100 mg/kg dose, inhibition at 24 hours (51%-78%) is almost comparable with that seen at 4 hours, and partial inhibition (25%-51%) persisted through 48 hours[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

541.02

Formula

C25H25ClN6O4S
CAS 号
性状

固体

颜色

Light yellow to yellow

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 : ≥ 100 mg/mL (184.84 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 1.8484 mL 9.2418 mL 18.4836 mL
5 mM 0.3697 mL 1.8484 mL 3.6967 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 (4.62 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 (4.62 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：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。
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， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.69%

COA (199 KB) LCMS (267 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

MCF7 human mammary carcinoma cells and PC-3 human prostate adenocarcinoma cells are maintained in culture conditions at 37°C under 5% CO2. For PI3K pathway status assessment following EGF treatment, the culture medium is replaced with test compounds dissolved in serum-free DMEM containing 0.3% DMSO. After incubation for 3 hours, cells are stimulated with 100 ng/mL of EGF for 10 minutes and Western immunoblot analysis of cell lysates is performed. Assessment of mTOR pathway status in Ramos cells is performed. Cellular proliferation is assessed using the Cell Proliferation ELISA, bromodeoxyuridine (BrdUrd) chemiluminescence kit. Cytotoxicity, apoptosis (caspases-3/7), anchorage-independent growth, and PC-3 cell migration assays are performed. Hepatocyte growth factor (HGF)-induced chemotaxis is assessed. Theendothelial cell tube formation assay is performed, with minor modifications. Total tube length is quantified with Image Pro Plus software[1].

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

Mice[1]
Female athymic nude mice and male nude mice are used. Tumor cells are cultured and established as xenografts in mice, and body and tumor weights assessed. Statistical significance is determined using the two-tailed Student ttest (significance defined as P<0.05). Pilaralisib (XL147) is formulated in sterile water/10 mmol/L HCl or water and administered at the indicated doses and regimens by oral gavage at a dose volume of 10 mL/kg.

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

Pilaralisib 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 1.8484 mL 9.2418 mL 18.4836 mL 46.2090 mL
5 mM 0.3697 mL 1.8484 mL 3.6967 mL 9.2418 mL
10 mM 0.1848 mL 0.9242 mL 1.8484 mL 4.6209 mL
15 mM 0.1232 mL 0.6161 mL 1.2322 mL 3.0806 mL
20 mM 0.0924 mL 0.4621 mL 0.9242 mL 2.3105 mL
25 mM 0.0739 mL 0.3697 mL 0.7393 mL 1.8484 mL
30 mM 0.0616 mL 0.3081 mL 0.6161 mL 1.5403 mL
40 mM 0.0462 mL 0.2310 mL 0.4621 mL 1.1552 mL
50 mM 0.0370 mL 0.1848 mL 0.3697 mL 0.9242 mL
60 mM 0.0308 mL 0.1540 mL 0.3081 mL 0.7702 mL
80 mM 0.0231 mL 0.1155 mL 0.2310 mL 0.5776 mL
100 mM 0.0185 mL 0.0924 mL 0.1848 mL 0.4621 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pilaralisib934526-89-3XL-147 SAR245408XL147XL 147SAR245408SAR 245408SAR-245408PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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