化合物OTX008 T16413

Product Introduction
Bioactivity


英文名: OTX008

描述: OTX008 (PTX008) 是半乳糖凝集素 1 选择性抑制剂。

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].

体内活性: OTX008治疗与治疗肿瘤中的Gal1和Ki67下调、微血管密度降低及VEGFR2表达减少相关。OTX008抑制A2780-1A9异种移植瘤的生长。联合研究表明，OTX008与多种细胞毒性和靶向治疗药物协同作用，尤其是当OTX008首先给药时[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mg/mL (10.67 mM)
Ethanol : 33.33 mg/mL (35.56 mM)


关键字: OTX 008 | OTX-008 | PTX-008 | Galectin | Calixarene0118 | inhibit | OTX008 | Calixarene-0118 | PTX 008 | Inhibitor

相关产品: G3-C12 acetate(848301-94-0 free base) | DB21, Galectin-1 Antagonist | Galectin-3/galectin-8-IN-1 | GB1107 | TD139 | Galectin-3/galectin-8-IN-2 | Thiodigalactoside | Galectin-3 antagonist 2

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途