化合物GDC-0575 T7300

Product Introduction
Bioactivity


英文名: GDC-0575

描述: GDC-0575 (ARRY-575) 是一种高选择性，有口服活性的小分子Chk1抑制剂，IC50值为1.2 nM。

动物实验: For in vivo experiments, aliquots of GDC-0575 (10 mg/mL) were stored at ?20℃and diluted in 100 mM sodium citrate buffer immediately prior to each experiment. GDC-0575 was used at 1.8 mg/ml for female mice (~25 g) and 2.6 mg/ml for male mice (~35 g) via oral gavage (final concentration 7.5 mg/kg). For in vitro experiments, aliquots of GDC-0575 (100 μM) were stored at ?20 ℃ and used at a final concentration of 100 nM. AraC (Cytosine β-D-arabinofuranoside C1768, Sigma) was used at 10 mg/kg (commonly used in clinical practice) for in vivo and at 100 nM and 500 nM for in vitro experiments. For in vivo experiments, toxicity of GDC-0575 was assessed in non-engrafted NSG mice using a range of concentrations of GDC-0575 in combination with AraC. 7.5 mg/kg GDC-0575 was the highest concentration to have no significant or lasting adverse effects in mice. Similarly, for in vitro experiments, 100 nM GDC-0575 in combination with 500 nM AraC was the highest concentration non-cytotoxic to MS5 stoma cell. ATR inhibitor was used at a final concentration of 0.5 μM[2].

体外活性: 相较于V158411、LY2603618和MK-8776，GDC-0575在促进DNA损伤、复制应激和细胞死亡方面在一组黑色素瘤细胞系中显示出显著更高的效力[1]。

体内活性: CHK1 inhibitor (CHK1i) GDC-0575 enhances AraC-mediated killing of AML cells both in vitro and in vivo, thus abrogating any potential chemoresistance mechanisms involving DNA repair. Importantly, this combination of drugs does not affect normal long-term hematopoietic stem/progenitors[2].

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

溶解度: DMSO : 50 mg/mL (132.18 mM)


关键字: RG 7741 | GDC-0575 | RG-7741 | GDC0575 | ARRY575 | inhibit | Inhibitor | Checkpoint Kinase (Chk) | ARRY 575 | GDC 0575

相关产品: A-443654 | BX-912 | MBM-55 | PF 477736 | SAR-020106 | Prexasertib dihydrochloride | GNE-900 | LY2880070 | Tuvusertib | BX795

相关库: Drug Repurposing Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Hematonosis 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