1. PI3K/Akt/mTOR
  2. PI3K mTOR
  3. PI3K/mTOR Inhibitor-4

PI3K/mTOR Inhibitor-4 

目录号: HY-128333 纯度: 97.00%
COA 产品使用指南

PI3K/mTOR Inhibitor-4 是一种泛 I 类 PI3K/mTOR 抑制剂,具有口服活性。PI3K/mTOR Inhibitor-4 对 PI3Kα、PI3Kγ、PI3Kδ 和 mTOR 具有酶抑制活性,IC50 值分别为 0.63 nM、22 nM、9.2 nM 和 13.85 nM。PI3K/mTOR Inhibitor-4 可用于癌症的研究。

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PI3K/mTOR Inhibitor-4 Chemical Structure

PI3K/mTOR Inhibitor-4 Chemical Structure

CAS No. : 2361215-32-7

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer[1].

IC50 & Target[1]

PI3Kα

0.63 nM (IC50)

PI3Kδ

9.2 nM (IC50)

mTOR

13.85 nM (IC50)

PI3Kβ

94.54 nM (IC50)

PI3Kγ

22 nM (IC50)

体外研究
(In Vitro)

PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively[1].
PI3K/mTOR Inhibitor-4 (2.5-10 µM; 24 h) inhibits the PI3K/AKT/mTOR pathway[1].

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

Cell Viability Assay[1]

Cell Line: PC12 and LO2 cells
Concentration: 0.625-20 µM
Incubation Time: 72 h
Result: Showed low toxicity in concentrations from 0.625 µM to 20 µM.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 2.5, 5 and 10 µM
Incubation Time: 24 h
Result: Dose-dependently decreased the level of phosphorylation of AKT and its downstream target S6 in Hela cell line.
体内研究
(In Vivo)

PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague−Dawley rats[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity[1].

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

Animal Model: SD rats (male; 200-220 g)[1]
Dosage: 1, 10 mg/kg
Administration: Intravenous, oral
Result:
IV (1 mg/kg) PO (10 mg/kg)
CL (ml/min/kg) Vss (ml/kg) Tmax (h) Cmax (ng/ml) AUCinf (ng*h/ml) t1/2 (h) F(%)
8.6 1199.81 2.67 886.67 4753.35 1.78 24.1
Animal Model: BALB/c nude mice (female; 6-7 weeks; 18-22 g)[1]
Dosage: 10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model)
Administration: Oral
Result: Inhibited the growth of xenograft tumors in a dose-dependent manner.
分子量

535.54

Formula

C27H22FN3O6S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (466.82 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 1.8673 mL 9.3364 mL 18.6727 mL
5 mM 0.3735 mL 1.8673 mL 3.7345 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 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

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

PI3K/mTOR Inhibitor-4 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, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8673 mL 9.3364 mL 18.6727 mL 46.6819 mL
5 mM 0.3735 mL 1.8673 mL 3.7345 mL 9.3364 mL
10 mM 0.1867 mL 0.9336 mL 1.8673 mL 4.6682 mL
15 mM 0.1245 mL 0.6224 mL 1.2448 mL 3.1121 mL
20 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3341 mL
25 mM 0.0747 mL 0.3735 mL 0.7469 mL 1.8673 mL
30 mM 0.0622 mL 0.3112 mL 0.6224 mL 1.5561 mL
40 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1670 mL
50 mM 0.0373 mL 0.1867 mL 0.3735 mL 0.9336 mL
60 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7780 mL
80 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 mL
100 mM 0.0187 mL 0.0934 mL 0.1867 mL 0.4668 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.

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PI3K/mTOR Inhibitor-4
目录号:
HY-128333
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