Palomid 529 是一种有效的 mTORC1 和 mT

Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.

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^[1]. 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 days compared with the control^[2]. Palomid 529 (P529) is able to reduce tumor growth in a dose-dependent manner both in PC3 and 22rv1 xenografts. A 10, 47.6, and 59.3% reduction of tumor mass is demonstrated in mice bearing PC3 xenografts receiving 50, 100, and 200 mg/kg Palomid 529 respectively and a 9, 38.7, and 51.5% reduction of tumor mass in mice bearing 22rv1 xenografts receiving 50, 100, and 200 mg/kg Palomid 529 respectively^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

406.43

Solid

C₂₄H₂₂O₆

914913-88-5

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (246.04 mM; Need ultrasonic)

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• 1.

  请依序添加每种溶剂： 10% DMSO 90% corn oil

  Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

• [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. [Content Brief]

  [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. [Content Brief]

  [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. [Content Brief]