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LY294002 抑制剂

参  考  价:650 - 950
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  • 型号

    HY-10108

  • 品牌

    MCE

  • 厂商性质

    代理商

  • 所在地

    杭州市

规格

10 mM * 1 mL in DMSO 715元 10000可售

5 mg 650元 10000可售

10 mg 950元 10000可售

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更新时间:2023-05-23 15:33:10浏览次数:544次

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产地 进口 级别 其他
LY294002 抑制剂
LY294002 是一种广谱 PI3K 抑制剂,抑制 PI3Kα, PI3Kδ 和 PI3Kβ 的 IC50 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 抑制剂 

注:本产品仅用于科研,不可用于临床

生物活性

LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively[1]. LY294002 also inhibits CK2 with an IC50 of 98 nM[2]. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator[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].

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

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.
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].

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

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°C, 6 months; -20°C, 1 month。-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。

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-CD in 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


  • 4.


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

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


  • 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





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