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] |
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| 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) |
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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. |
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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. |
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| 運(yùn)輸條件 | Room temperature in continental US; may vary elsewhere. |
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| 儲(chǔ)存方式 | | Powder | -20°C | 3 years |
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| 4°C | 2 years |
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| In solvent | -80°C | 6 months |
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| -20°C | 1 month |
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| 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 |
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| 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(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
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