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LY294002 抑制劑

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  • 型號

    HY-10108

  • 品牌

    MCE

  • 廠商性質(zhì)

    代理商

  • 所在地

    杭州市

規(guī)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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LY294002 抑制劑
LY294002 是一種廣譜 PI3K 抑制劑，抑制 PI3Kα, PI3Kδ 和 PI3Kβ 的 IC50 分別為 0.5, 0.57, 0.97 μM。LY294002 也可抑制 CK2 的活性，IC50 為 98 nM。LY294002 是一種競爭性 DNA-PK 抑制劑，可逆結(jié)合 DNA-PK 的激酶結(jié)構(gòu)域，IC50 為 1.4 μM

LY294002 抑制劑 

注：本產(chǎn)品僅用于科研，不可用于臨床

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)

體外研究
(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.
體內(nèi)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

性狀

Solid

Formula

C19H17NO3

CAS 號

154447-36-6

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month
溶解性數(shù)據(jù)
In Vitro:

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

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

配制儲備液
濃度溶劑體積質(zhì)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
*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

請根據(jù)您的實驗動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨?。以下溶解方案都請先按?In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 1.


    請依序添加每種溶劑： 0.5% CMC-Na/saline water

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


  • 2.


    請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in saline)

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


  • 3.


    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

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


  • 4.


    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

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


  • 5.


    請依序添加每種溶劑： 10% DMSO    90% corn oil

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





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