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LY294002
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY294002图片
CAS NO:154447-36-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议
5 g电议

产品介绍
LY294002 是一种广谱PI3K抑制剂,抑制PI3Kα,PI3KδPI3KβIC50分别为 0.5, 0.57, 0.97 μM。LY294002 也可抑制CK2的活性,IC50为 98 nM。LY294002 是一种竞争性DNA-PK抑制剂,可逆结合 DNA-PK 的激酶结构域,IC50为 1.4 μM。LY294002 是一种凋亡 (apoptosis) 激活剂。
生物活性

LY294002 is a broad-spectrum inhibitor ofPI3KwithIC50s of 0.5, 0.57, and 0.97 μM forPI3Kα,PI3KδandPI3Kβ, respectively[1]. LY294002 also inhibitsCK2with anIC50of 98 nM[2]. LY294002 is a competitiveDNA-PKinhibitor that binds reversibly to the kinase domain ofDNA-PKwith anIC50of 1.4 μM. LY294002 is anapoptosisactivator[3].

IC50& Target[1][2][4]

p110α

0.5 μM (IC50)

p110δ

0.57 μM (IC50)

p110β

0.97 μM (IC50)

human CK2

98 nM (IC50)

human CK2α2

3.869 μM (IC50)

DNA-PK

1.4 μM (IC50)

体外研究
(In Vitro)

LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion[4].
LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent[4].
LY294002 (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration[4].
LY294002 (5, 10, 100 μM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 μM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels[6].

Cell Proliferation Assay[4]

Cell Line:CNE-2Z cells
Concentration:0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
Incubation Time:24 hours and 48 hours
Result:Decreased CNE-2Z cells in a dose-dependent fashion.

Apoptosis Analysis[4]

Cell Line:CNE-2Z cells
Concentration:0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
Incubation Time:24 hours and 48 hours
Result:Induced apoptosis rate in dose-dependent.

Western Blot Analysis[4]

Cell Line:CNE-2Z cells
Concentration:10 μM, 25 μM, 50 μM, and 75 μM
Incubation Time:
Result:Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group.
体内研究
(In Vivo)

LY294002 (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden[4].
LY294002 (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats[5].

Animal Model:Athymic nude mice (6-8 weeks) with CNE-2Z xenograft[4]
Dosage:10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg
Administration:Intraperitoneal injection; twice weekly, for 4 weeks
Result:Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.
分子量

307.34

性状

Solid

Formula

C19H17NO3

CAS 号

154447-36-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(162.69 mM;Need ultrasonic)

Ethanol : 50 mg/mL(162.69 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.2537 mL16.2686 mL32.5373 mL
5 mM0.6507 mL3.2537 mL6.5075 mL
10 mM0.3254 mL1.6269 mL3.2537 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 0.5%CMC-Na/saline water

    Solubility: 15.71 mg/mL (51.12 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 5% DMSO    95% (20%SBE-β-CDin saline)

    Solubility: 2.87 mg/mL (9.34 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (7.32 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (7.32 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (7.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。