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Palomid 529

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Chemical Structure| 914913-88-5 同义名 : P529;RES-529;SG 00529
CAS号 : 914913-88-5
货号 : A602029
分子式 : C24H22O6
纯度 : 99%+
分子量 : 406.428
MDL号 : MFCD18633224
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(258.35 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • mTORC1
描述 Palomid 529 (P529) inhibits endothelial cell proliferation driven by VEGF (IC50, 20 nM) and bFGF (IC50, 30 nM) and induces endothelial cell apoptosis[1]. Palomid 529 (RES-529) serves as a PI3K/AKT/mTOR pathway inhibitor, disrupting the pathway by dissociating both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2). This inhibitor reduces mTORC1/mTORC2 activity across various cancer cell lines, evidenced by decreased phosphorylation of ribosomal protein S6, 4E-BP1, and AKT, which leads to cell growth inhibition and cell death, typically within the 5-15 μM range. At a concentration of 10 μM, Palomid 529 diminishes the binding of 0.5 nM [3H]estradiol to estrogen receptor (ER)α and ERβ by 3% or less. It inhibits HUVEC cell proliferation induced by VEGF and β fibroblast growth factor, with IC50 values of approximately 10 and 30 nM, respectively. Palomid 529 also induces a four-fold increase in apoptosis in HUVEC cells, as indicated by DNA fragmentation. In various cancer cell lines from the National Cancer Institute-60 (NCI-60) tumor panel, Palomid 529 demonstrates growth inhibition with IC50 values ranging from 5-15 μM for central nervous system cancer cells and 5-30 μM for prostate cancer cells[2]. Palomid 529 (P529) leads to a dose- and time-dependent reduction in Akt activity in PC3, LnCaP, and 22rv1 cells, as indicated by decreased phosphorylation of Akt (Ser473). This effect is consistent across all PCa cells with enzymatic IC50s around 0.2 μM. Palomid 529 variably inhibits the proliferation of neoplastic cells (IC50s ranging from 5 to 28 μM), while having minimal impact on non-neoplastic BPH1 and EPN cells. Additionally, treatment with Palomid 529 causes a concentration-dependent decrease in the viability and proliferation
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL
参考文献

[1]Xue Q, et al. Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability. Cancer Res, 2008, 68(22), 9551-9557.

[2]Weinberg MA, et al. RES-529: a PI3K/AKT/mTOR pathway inhibitor that dissociates the mTORC1 and mTORC2 complexes. Anticancer Drugs. 2016 Jul;27(6):475-87.

[3]Gravina GL, et al. The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel andcisplatin in aggressive and hormone-refractory prostate cancer cells. Endocr Relat Cancer. 2011 Jul 1;18(4):385-400.