HY-10108-LY294002 抑制剂-杭州昊鑫生物科技股份有限公司手机版

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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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg	5 mg	10 mg

1 mM	3.2537 mL	16.2686 mL	32.5373 mL
5 mM	0.6507 mL	3.2537 mL	6.5075 mL
10 mM	0.3254 mL	1.6269 mL	3.2537 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

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

产品简介

详细介绍