Palomid 529 (P529)

別名:SG 00529

Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS. Phase 1.

Palomid 529 (P529)化学構造

CAS No. 914913-88-5

サイズ 価格(税別) 在庫状況
JPY 30200 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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製品安全説明書

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Palomid 529 (P529)関連製品

シグナル伝達経路

mTOR阻害剤の選択性比較

生物活性

製品説明 Palomid 529 (P529, SG 00529) inhibits both the mTORC1 and mTORC2 complexes, reduces phosphorylation of pAktS473, pGSK3βS9, and pS. Phase 1.
Targets
mTORC1 [1] mTORC2 [1]
In Vitro
In vitro

Palomid 529 inhibits proliferation and increases apoptosis of endothelial cells. Palomid 529 inhibits both VEGF-driven and bFGF-driven endothelial cell proliferation with IC50 of 20 nM and 30 nM, respectively. Palomid 529 retains the ability to induce endothelial cell apoptosis. Palomid 529 decreases VEGF-A–driven phosphorylation of pAktS473, pGSK3βS9, and pS6. However, Palomid 529 prevents neither phosphorylated mitogen-activated protein kinase (pMAPK) nor pAktT308 as potently as pAktS473.[1] Palomid 529 not only reduces the proliferative response in the ischemic retina but also improves the organization and structure of the vessels that form. [1] Palomid 529 shows a potent antiproliferative activity in the NCI-60 cell lines panel, with growth inhibitory 50 (GI50) <35 μM. In addition, Palomid 529 significantly enhances the antiproliferative effect of radiation in prostate cancer cells (PC-3). Palomid 529 gives rise to a concentration dependent growth inhibition on PC-3 cells. Doses of 2 and 7μM resulted in 30 and 60% growth inhibition, respectively. Palomid 529 inhibits the radiation-induced p-Akt activation and decreases Bcl-2/Bax ratio in PC-3. Palomid 529 not only inhibits radiation-induced overexpression of Id-1 and VEGF but also down-regulates radiation-induced MMP-2 and MMP-9. [2]

Kinase Assay Estrogen receptor binding assays
The proteins are produced with rabbit reticulocyte lysates. The amount of template used in each reaction is determined empirically and expression is monitored in parallel reactions where [35S]methionine is incorporated into the receptor followed by gel electrophoresis and exposure to film. Binding reactions of the estrogen receptors (ER) and Palomid 529 are carried out in 100 mL final volumes in TEG buffer [10 mM Tris (pH 7.5), 1.5 mM EDTA, 10% glycerol]. In vitro transcribed-translated receptor (5 μL) is used in each binding reaction in the presence of 0.5 nM [3H]estradiol (E2). Palomid 529 is routinely tested from 10−11 to 10−6 M and diluted in ethanol. The reactions are incubated at 4 °C overnight and bound E2 is quantified by adding 200 mL dextran-coated charcoal. After a 15-minutes rotation at 4 °C, the tubes are centrifuged for 10 minutes and 150 mL of the supernatant are added to 5 mL scintillation mixture for determination of cpm by liquid scintillation counting. The maximum binding is determined by competing bound E2 with only the ethanol vehicle. Controls for background are included in each experiment using 5 mL unprogrammed rabbit reticulocyte lysate. This value, typically 10% to 15% of the maximal counts, is subtracted from all values. The data are plotted and Ki values are calculated. Experiments are conducted at least thrice in duplicate.
細胞実験 細胞株 Human umbilical vascular endothelial cells (HUVEC)
濃度 ~20 μM
反応時間 48 hours
実験の流れ

Human umbilical vascular endothelial cells (HUVEC) are used. The proliferation assay is carried out by seeding the HUVECs in 96-well plates at a density of 1,000 per well in complete medium. Following a 24-hour plating period, the cells are starved for 24 hours in 0.5% serum before being treated with Palomid 529 in the presence of 10 ng/mL basic fibroblast growth factor (bFGF) or VEGF in complete medium. After 48 hours, cell number is determined using a colorimetric method. The results are expressed as the percentage of the maximal bFGF or VEGF response in the absence of Palomid 529. Nonproliferating endothelial cells are assayed by growing HUVECs to quiescence in 96-well plates and treating with Palomid 529 for 48 hours. Initially, 5,000 cells per well are seeded and confluence is achieved the next day. The plates are incubated for another 24 hours to ensure growth arrest before treatment with Palomid 529.

In Vivo
In Vivo

Palomid 529 shows a dose-dependent inhibition of the Ad-VEGF-A–driven angiogenesis following Palomid 529 treatment. Palomid 529 inhibits C6V10 glioma tumor growth in nude mice following i.p. dosing. Palomid 529 decreases AktS473 but not AktT308 signaling. Palomid 529 inhibits C6V10 glioma tumor growth in nude mice following i.p. dosing. Palomid 529 decreases AktS473 but not AktT308 signaling. Palomid 529 inhibits tumor growth, angiogenesis, and vascular permeability. [1] Treatment of PC-3 tumour-bearing mice with Palomid 529 reduced tumour growth to 57.1% compared with controls. [2] Palomid 529 is an effective suppressor of Müller cell proliferation, glial scar formation, and photoreceptor cell death in a rabbit model of retinal detachment (RD). [3] Palomid 529 significantly suppresses Brca1-deficient tumor growth in mice through inhibition of both Akt and mTOR signaling. [4]

化学情報

分子量 406.43 化学式

C24H22O6

CAS No. 914913-88-5 SDF Download Palomid 529 (P529) SDFをダウンロードする
Smiles CC(C1=CC2=C(C=C1)C3=CC(=C(C=C3OC2=O)OCC4=CC=C(C=C4)OC)OC)O
保管

In vitro
Batch:

DMSO : 81 mg/mL ( (199.29 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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