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產(chǎn)地	進(jìn)口	級(jí)別	其他

注：本產(chǎn)品僅用于科研，不可用于臨床

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(jìng)爭(zhēng)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 是一種凋亡 (apoptosis) 激活劑。

LY294002抑制劑生物活性

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(hào)

154447-36-6

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(chǔ)備液

濃度溶劑體積質(zhì)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

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊?qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)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(qǐng)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(qǐng)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(qǐng)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(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution