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

Voxtalisib  (Synonyms: XL765; SAR245409)

目录号: HY-15900 纯度: 98.81%
COA 产品使用指南

摩尔计算器

Voxtalisib (XL765) 是一种有效的 PI3K 抑制剂，抑制p110α，p110β，p110γ 和 p110δ，IC50 分别为 39, 113, 9 和 43 nM，也抑制 DNA-PK (IC50=150 nM) 和 mTOR (IC50=157 nM)。Voxtalisib (XL765) 抑制 mTORC1 和 mTORC2，IC50s 分别为 160 和 910 nM。

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Voxtalisib Chemical Structure

Voxtalisib Chemical Structure

CAS No. : 934493-76-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1238
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2 mg ￥833
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5 mg ￥1250
In-stock
10 mg ￥1950
In-stock
25 mg ￥3950
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Voxtalisib 相关抗体

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查看 PI3K 亚型特异性产品:

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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

Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.

IC50 & Target[1][2]

p110γ

9 nM (IC50)

p110α

39 nM (IC50)

p110δ

43 nM (IC50)

p110β

113 nM (IC50)

mTOR

157 nM (IC50)

mTORC1

160 nM (IC50)

mTORC2

910 nM (IC50)

DNA-PK

150 nM (IC50)

体外研究
(In Vitro)

Voxtalisib (XL765) displays potent inhibitory activity against class I PI3K isoforms p110α, p110β, p110δ, and p120γ, with IC50s of 39, 110, 43, and 9 nM, respectively. The IC50 value for inhibition of PI3Kα by Voxtalisib is determined at various concentrations of ATP, revealing Voxtalisib be an ATP-competitive inhibitor with an equilibrium inhibition constant (Ki) value of 13 nM. Voxtalisib also inhibits mTOR (IC50s of 160 and 910 nM for mTORC1 and mTORC2, respectively) in an immune-complex kinase assay and the PI3K-related kinase DNA-PK (IC50 value of 150 nM). In contrast, Voxtalisib (XL765) has relatively weak inhibitory activity toward the class III PI3K vacuolar sorting protein 34 (VPS34; IC50 value of ~9.1 μM). Consistent with its inhibitory activity against purified PI3K proteins, SAR245409 inhibits EGF-induced PIP3 production in PC-3 and MCF7 cells with IC50s of 290 and 170 nM, respectively. The ability of Voxtalisib 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 by cell-based ELISA. Voxtalisib inhibits these activities with IC50s of 250 and 120 nM, respectively. In MCF7 and PC-3 cells, Voxtalisib inhibits proliferation (monitored by BrdUrd incorporation) with IC50s of 1,070 and 1,840 nM, respectively. To further characterize the effects of Voxtalisib on tumor cell growth, an assay monitoring the anchorage-independent growth of PC-3 and MCF7 cells in soft agar over a 14-day period is used. SAR245409 inhibits colony growth with an IC50 value of 270 nM in PC-3 cells and 230 nM in MCF7 cells[2].

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

Voxtalisib 相关抗体:
体内研究
(In Vivo)

Oral administration of Voxtalisib (XL765) causes a dose-dependent decrease of phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 84% inhibition of S6 phosphorylation at 30 mg/kg at 4 hours. The dose-response relationships derive from the 4 hours time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation to occur at doses of 19 mg/kg (pAKTT308 and pAKTS473), 51 mg/kg (p-p70S6K), and 18 mg/kg (pS6). Inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 30 mg/kg dose of Voxtalisib is maximal at 4 hours, reaching 61% to 84%; however, the level of inhibition decreases to 0% to 42% by 24 hours, and minimal or no inhibition is evident by 48 hours. Following a 100 mg/kg dose of Voxtalisib, inhibition is also maximal at 4 hours (52%-75%)[2].

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

270.29

Formula

C13H14N6O
CAS 号
性状

固体

颜色

Off-white to brown

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 : 10 mg/mL (37.00 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6997 mL 18.4986 mL 36.9973 mL
5 mM 0.7399 mL 3.6997 mL 7.3995 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: ≥ 1 mg/mL (3.70 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (3.70 mM); 澄清溶液

    此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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: 98.81%

COA (193 KB) LCMS (274 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

Cellular proliferation is assessed using the Cell Proliferation ELISA, Bromodeoxyuridine Chemiluminescence Kit. Cytotoxicity is assessed using the ATP Bioluminescence Assay as follows: PC-3, MCF7, A549, LS174T, MDA-MB-468, U87-MG, and OVCAR-3 cells are plated at densities of 7×103, 1.5×104, 6×103, 7×103, 7×103, 6×103, 1.5×104 cells per well, respectively, onto 96-well microtiter plates in culture medium, incubated at 37°C, 5% CO2 for 18 hours, and then treated with a serial dilution of compound in medium containing a final concentration of 0.3% DMSO. Triplicate wells are used for each compound concentration. Control wells receive 0.3% DMSO in media. Cultures are incubated at 37°C, 5% CO2 for an additional 24 hours and cells are then assayed for viability using the ViaLight HS Kit[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
In vivo efficacy studies are performed in athymic nude mice. Tumor cells are cultured in DMEM supplemented with 10% FBS (20% for PC-3 and OVCAR-3 cells), Penicillin-Streptomycin, and nonessential amino acids at 37°C in a humidified 5% CO2 atmosphere. On day 0, cells are harvested by brief trypsinization, and 1 to 5×106 cells in 0.1 mL ice-cold Hanks Balanced Salt Solution are implanted subcutaneously (OVCAR-3) or intradermally (MCF7 and U-87 MG) into the hind flank of female athymic nude mice. In the case of the MCF7 model, an estrogen pellet (IRA) is implanted subcutaneously at the nape of neck at the time of tumor cell implantation. A total of 3×106 PC-3 cells are similarly harvested and implanted subcutaneously into the hind-flank of 5- to 8-week-old male nude mice. Tumor growth is monitored weekly with calipers until staging and dose initiation. During the dosing period, body and tumor weights are assessed. Voxtalisib (XL-765) is formulated in sterile water/10 mM 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

Voxtalisib 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 3.6997 mL 18.4986 mL 36.9973 mL 92.4932 mL
5 mM 0.7399 mL 3.6997 mL 7.3995 mL 18.4986 mL
10 mM 0.3700 mL 1.8499 mL 3.6997 mL 9.2493 mL
15 mM 0.2466 mL 1.2332 mL 2.4665 mL 6.1662 mL
20 mM 0.1850 mL 0.9249 mL 1.8499 mL 4.6247 mL
25 mM 0.1480 mL 0.7399 mL 1.4799 mL 3.6997 mL
30 mM 0.1233 mL 0.6166 mL 1.2332 mL 3.0831 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:

Voxtalisib934493-76-2XL765 SAR245409XL 765XL-765SAR245409SAR 245409SAR-245409PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinInhibitorinhibitorinhibit

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