LY294002

製品コードS1105 バッチS110506

印刷

化学情報

Chemical Structure Synonyms SF 1101, NSC 697286 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H17NO3
分子量 307.34 CAS No. 154447-36-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 61 mg/mL (198.47 mM)
Ethanol 61 mg/mL (198.47 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%absolute ethyl alcohol 95%Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.000mg/ml (3.25mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear absolute ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓ を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。
in vitro

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. This compound is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1[5]. It inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. This chemical demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]It induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, this compound markedly inhibits ovarian cancer cell proliferation in vitro. It 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 this chemical on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
in vivo

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] This compound significantly inhibits growth and ascites formation of ovarian carcinoma. [3]

プロトコル(参考用のみ)

キナーゼアッセイ 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. This compound is tested against the Upstate panel of kinases in 10 μM ATP.
細胞アッセイ 細胞株 Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
濃度 0–50 μM
反応時間 0–48 hours
実験の流れ

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 動物モデル Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
投薬量 0–100 mg/kg
投与方法 Administered via i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17362206/
  • https://pubmed.ncbi.nlm.nih.gov/12060641/
  • https://pubmed.ncbi.nlm.nih.gov/10741711/
  • https://pubmed.ncbi.nlm.nih.gov/17302559/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1868829/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3560216/

カスタマーフィードバック

Data from [Data independently produced by Int J Biochem Cell Biol, 2015, 60, 34-42]

Data from [Data independently produced by Hum Reprod, 2015, 30(2), 284-98]

Data from [Data independently produced by Sci Rep, 2015, 5, 11634]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The intrinsic expression of NLRP3 in Th17 cells promotes their protumor activity and conversion into Tregs [ Cell Mol Immunol, 2025, 22(5):541-556] PubMed: 40195474
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WNK1 mediates M-CSF-induced macropinocytosis to enforce macrophage lineage fidelity [ Nat Commun, 2025, 16(1):4945] PubMed: 40436823
X-linked myopathy with excessive autophagy: characterization and therapy testing in a zebrafish model [ EMBO Mol Med, 2025, 10.1038/s44321-025-00204-8] PubMed: 39994482
Exosomes derived from platelet-rich plasma alleviate synovial inflammation by enhancing synovial lymphatic function [ J Nanobiotechnology, 2025, 23(1):522] PubMed: 40671121
PDPN+ cancer-associated fibroblasts enhance gastric cancer angiogenesis via AKT/NF-κB activation and the CCL2-ACKR1 axis [ MedComm (2020), 2025, 6(1):e70037] PubMed: 39764562
Junctional adhesion molecule A orchestrates endothelial cell-driven angiogenesis and wound healing in diabetes [ Pharmacol Res, 2025, 217:107796] PubMed: 40436082
Matrix stiffness regulates glucose-6-phosphate dehydrogenase expression to mediate sorafenib resistance in hepatocellular carcinoma through the ITGB1-PI3K/AKT pathway [ Cell Death Dis, 2025, 16(1):538] PubMed: 40685383
APJ regulates the balance between self-renewal and differentiation of vascular endothelial stem cells [ Inflamm Regen, 2025, 45(1):25] PubMed: 40760447
Active R-RAS2/TC21 prevents cell cycle arrest and morphological alterations in mouse embryonic fibroblasts lacking RAS proteins [ Oncogene, 2025, 10.1038/s41388-025-03367-3] PubMed: 40164870

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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