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OTX008

OTX008 (PTX008) 是半乳糖凝集素 1 选择性抑制剂。

CAS号

286936-40-1

分子式

C52H72N8O8

主要靶点

Galectin

仅限科研使用

Cat No : CM04221

Print datasheet

Synonyms

PTX008|Calixarene 0118

验证数据展示

  • CAS No.: 286936-40-1

    OTX008
    CAS#: 286936-40-1

产品信息

OTX008 is a selective galectin-1 inhibitor.

CAS号 286936-40-1
分子式 C52H72N8O8
主要靶点 Galectin
主要通路 免疫与炎症
分子量 937.18
纯度 98.55%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 PTX008|Calixarene 0118

体内活性

OTX008 treatment is associated with the down-regulation of Gal1 and Ki67 in treated tumors, as well as decreased microvessel density and VEGFR2 expression. OTX008 inhibits the growth of A2780-1A9 xenografts. Combination studies display OTX008 synergy with several cytotoxic and targeted therapies, principally when OTX008 is administered first[1].

体外活性

OTX008 inhibits Gal1 expression and ERK1/2 and AKT-dependent survival pathways in SQ20B and A2780-1A9 cells and induces G2/M cell cycle arrest through CDK1. OTX008 increases the anti-proliferative effects of Semaphorin-3A (Sema3A) in SQ20B cells and reverses invasion induced by exogenous Gal1. Growth inhibitory concentrations (GI50) of OTX008 range from 3 to 500 μM in a large panel of human solid tumor cell lines. A significant correlation between OTX008 GI50 values and Gal1 mRNA (LGALS1) and protein expression levels in the panel of cancer cells is observed. OTX008 affects endothelial cell proliferation, motility, invasiveness, and cord formation. Tumor cell proliferation is also inhibited, with differences in sensitivity among cell lines (IC50 from 1 to 190 μM)[1][2].

溶解度

Ethanol:33.33 mg/mL (35.56 mM),DMSO:10 mg/mL (10.67 mM),Sonification is recommended.

参考文献

1.Astorgues-Xerri L, et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis. Eur J Cancer. 2014 Sep;50(14):2463-77.
2.Zucchetti M, et al. Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib. Cancer Chemother Pharmacol. 2013 Oct;72(4):879-87.

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