LY294002 化学構造
分子量: 307.34

品質と確認

製品表彰状(43)

カスタマーレビュー(10)

Quality Control & MSDS

製品情報

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  • 研究分野
  • LY294002のメカニズム

製品の説明

生物活性

情報 LY294002は、p110α、p110δとp110βのPI3K阻害剤で、IC50 がそれぞれ 0.5 μM、0.57 μM、0.97 μMです。
目標 p110α p110δ p110β
IC50 0.5 μM 0.57 μM 0.97 μM[1]
In vitro試験 LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
In vivo試験 LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]
臨床試験 LY294002 is currently in Phase I clinical trials in patients with cancers.
特集

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [4]

kinase assays PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.

細胞アッセイ: [2]

細胞系 Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
濃度 0–50 μM
処理時間 0–48 hours
方法 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.

動物実験: [3]

動物モデル Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
製剤 Dissolved in DMSO plus 0.25 ml of PBS
投薬量 0–100 mg/kg
管理 Administered via i.p.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download LY294002 SDF
分子量 307.34
化学式

C19H17NO3

CAS No. 154447-36-6
保管 2年-20℃
6月-80℃in DMSO
別名 SF 1101, NSC 697286
溶解度 (25°C) * In vitro DMSO 36 mg/mL (117.13 mM)
<1 mg/mL (<1 mM)
エタノール 21 mg/mL (68.32 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 2-morpholino-8-phenyl-4H-chromen-4-one

研究分野

カスタマーレビュー (10)


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Source Hepatology, 2014, 59(4), 1262-72. LY294002 purchased from Selleck
Method Immunoblot analysis
Cell Lines Huh7 cells
Concentrations
Incubation Time 6 h
Results Ly294002, SB203580, rottlerin, PD98059, and SP600125 were applied to Huh7 cells to specifically inhibit the activities of p38 MAPK, PKC-d, PI3K, MEK, and JNK, respectively, and the cells were subsequently stimulated with either IFN-a or IFN-b for the next 6 hours. Overall, PKC-d was found to be primarily responsible for S727 phosphorylation in the signaling pathways of both type I IFNs, with the kinase inhibitor rottlerin blocking a majority of the serine phosphorylation after 6 hours of stimulation.

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Source Oncogene, 2012, 31, 3277–3286. LY294002 purchased from Selleck
Method Western Blot
Cell Lines HEK-293 cells
Concentrations 30 uM
Incubation Time
Results We cultured HEK-293 cellsstably overexpressing p37d or p110d with the general PI3K –inhibitor, LY294002, or the MAPK-inhibitor, AZD6244. The inhibitors strongly affected the levels ofphosphorylated AKT S473 and ERK.

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Source Clin Cancer Res, 2011, 17, 7116-7126. LY294002 purchased from Selleck
Method Western blot
Cell Lines FaDu cells
Concentrations 20 μmol/L
Incubation Time 0-30 min
Results Both BGT226 and LY294002 attenuated p-AKT and p-p70 Thr389 expression after short-term treatment, whereas rapamycin diminished the phosphorylation of p70S6K but not AKT.

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Source Mol Oncol, 2013, 7, 359-68. LY294002 purchased from Selleck
Method Xenograft
Cell Lines SCC61, Detroit 562
Concentrations 100 mg/kg
Incubation Time 20 day
Results In female nude mice injected with SCC61 or Detroit 562 cells, both gefitinib and LY294002 inhibited tumor growth (Figure 5). However, the most effective way to inhibit tumor growth in EGFR resistant cell line tumors in vivo was to block both EGFR and PI3K activity with gefitinib and LY294002.

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Source Mol Oncol, 2013, 7, 359-68. LY294002 purchased from Selleck
Method Cell growth inhibition assay with MTT
Cell Lines SQ20B/SCC61/SCC35/SCC25/HN31/MSK921/Detroit 562/HN5 cell
Concentrations 10 uM
Incubation Time 4 h
Results LY294002 effectively reduced cell viability while the combination of LY294002 and gefitinib had an additive effect (Figure A).

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Source Br J Pharmacol, 2013, 70(5), 1137-51. LY294002 purchased from Selleck
Method Immunofluorescence
Cell Lines MCF-7 FLV1000 cells
Concentrations 2/4 uM
Incubation Time 16 h
Results The involvement of PTEN/PI3K/Akt pathway in the internalization of ABCG2 by PPARγ agonists was further examined by the use of PI3K inhibitor (LY294002). As illustrated in Figure, treatment of MCF-7 FLV1000 by LY294002 for 16 h was found to cause concentration-dependent translocation of ABCG2 from plasma membrane to the subcellular compartment, mirroring the effect of the three PPARγ agonists.

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Source Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck
Method Immunofluorescence
Cell Lines HC11 cells
Concentrations 50 μM
Incubation Time 1 h
Results whole ADRP levels, estimated by Western blot , decreased only in the presence of MK -2206 and LY294002. In most cases, ADRP decorated the surface of small lipid droplets and appeared as little patches on large cytoplasmic lipid droplets. With the exception of SP600125, which induced a strong ADRP coating of almost all cytoplasmic lipid droplets (although this inhibitor did not increase ADRP synthesis), variation in the distribution of ADRP at the surface of lipid droplet was difficult to estimate, notably because the signal was faint and uneven.

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Rating
Source Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck
Method Western blot
Cell Lines HC11 cells
Concentrations 50 μM
Incubation Time
Results Addition of 50μM LY294002, a PI3-kinase inhibitor with higher stability and specificity provoked the complete arrest of PRL-induced β-casein synthesis and a drastic inhibition of that of ADRP.

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Rating
Source 2010, Saraswati Sukumar of Johns Hopkins University School of Medicine. LY294002 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations
Incubation Time 1 h
Results Reduction of AKT phosphorylation in T47D cells treated with LY294002 was observed.

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Rating
Source 2010, Dr. Zhang of Tianjin Medical University. LY294002 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 0.1-20 μM
Incubation Time 24 h
Results Reduction of AKT phosphorylation in T47D cells treated with LY294002 was observed.

製品表彰状 (43)

技術サポート&よくある質問(FAQ)

顧客がするかもしれない質問に対する答えは、指示を取り扱っている阻害剤で見つかります。話題は、貯蔵液(阻害剤と特別な注意を細胞ベースの分析法と動物のために必要とする問題を保存することは実験します)を準備する方法を含みます。

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