Palomid 529 (Synonyms: P529)
目录号: PL04132 纯度: ≥99%
CAS No. :914913-88-5
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PL04132-5mg 5mg ¥1260.00 请登录
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PL04132-50mg 50mg ¥9275.00 请登录
PL04132-100mg 100mg ¥8036.00 请登录
PL04132-200mg 200mg 询价 询价
PL04132-500mg 500mg 询价 询价
PL04132-10mM*1mLinDMSO 10mM*1mLinDMSO ¥1060.00 请登录
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中文名称
Palomid 529
中文别名
8-(1-羟基乙基)-2-甲氧基-3-[(4-甲氧基苯基)甲氧基]-6H-二苯并[B,D]吡喃-6-酮;Palomid 529 (P529) 抑制剂
英文名称
Palomid 529
英文别名
Palomid 529;Palomid 529 (P529);8-(1-Hydroxyethyl)-2-methoxy-3-((4-methoxybenzyl)oxy)-6H-benzo[c]chromen-6-one;8-(1-hydroxyethyl)-2-methoxy-3-[(4-methoxyphenyl)methoxy]benzo[c]chromen-6-one;P529;P-529;Palomid 529,P529;Palomid-529;8-(1-Hydroxyethyl)-2-methoxy-3-[(4-methoxyphenyl)methoxy]-6H-dibenzo[b,d]pyran-6-one;SG 00529;Palomid529;AK160239;8-(1-hydroxyethyl)-2-methoxy-3-(4-methoxybenzyloxy)-6H-benzo[c]chromen-6-one;6H-Dibenzo(b,d)pyran-6-one, 8-(1-hydroxyethyl)-2-methoxy-3-((4-methoxyphenyl)methoxy)-;6H-Dibenzo[b,d]pyran-6-one, 8-(1-hydroxyethyl)-2-methoxy-3;8-(1-Hydroxyethyl)-2-methoxy-3-[(4-methoxyphenyl)methoxy]-6H-dibenzo[b,d]pyran-6-one (ACI);8-(1-hydroxyethyl)-2-methoxy-3-(4-methoxybenzyloxy)-benzo[c]chromen-6-one;DFN 529;P 529;RES 529
Cas No.
914913-88-5
分子式
C24H22O6
分子量
406.43
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Palomid 529 是一种有效的 mTORC1 和 mTORC2 复合体抑制剂。
生物活性
Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.
性状
Solid
IC50 & Target[1][2]
TORC1 TORC2
体外研究(In Vitro)
Palomid 529 (P529) inhibits both VEGF-driven (IC50, 20 nM) and bFGF-driven (IC50, 30 nM) endothelial cell proliferation and retained the ability to induce endothelial cell apoptosis. Palomid 529 (RES-529) is a PI3K/AKT/mTOR pathway inhibitor that interferes with the pathway through both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) dissociation. Palomid 529 inhibits mTORC1/mTORC2 activity in various cancer cell lines, as noted by decreased phosphorylation of substrates including ribosomal protein S6, 4E-BP1, and AKT, leading to cell growth inhibition and death, with activity generally in the range of 5-15 μM. At 10 μM concentrations, Palomid 529 reduces the binding of 0.5 nM [H]estradiol to estrogen receptor (ER)α and ERβ by 3% or less. Palomid 529 inhibits both VEGF-stimulated and β fibroblast growth factor-stimulated HUVEC cell proliferation with
体内研究(In Vivo)
Palomid 529 (200 mg/kg/2d) inhibits C6V10 glioma tumor growth in nude mice following i.p. dosing. Analysis of signaling within the tumor lysates reveals that Palomid 529 (P529) also reduces AktS473 but not AktT308 signaling. Palomid 529 (RES-529) has shown antitumor activity in a variety of mouse models, including those for glioblastoma, and prostate and breast cancer. In a C6V10 glioblastoma subcutaneous xenograft model, mice pretreated with Palomid 529 (200 mg/kg/2 days, intraperitoneal) 1 week before and for 3 weeks after a tumor cell injection showed an ~70% decrease in tumor volume compared with the control. In another glioblastoma tumor model using human U87 cells, mice treated with micronized Palomid 529 3 days after a tumor cell injection showed a reduction in tumor growth by ~78 and 29% with 50 and 25 mg/kg/2 days, intraperitoneal, Palomid 529, respectively, after 24
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (246.04 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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