| Name | GDC-0575 |
| Description | GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM). |
| Animal Research | 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]. |
| In vitro | GDC-0575 demonstrates markedly higher efficacy in inducing DNA damage, replication stress, and cell death compared to V158411, LY2603618, and MK-8776 in a panel of melanoma cell lines[1]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (132.18 mM)
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| Keywords | RG 7741 | GDC-0575 | RG-7741 | GDC0575 | ARRY575 | inhibit | Inhibitor | Checkpoint Kinase (Chk) | ARRY 575 | GDC 0575 |
| Inhibitors Related | Rabusertib | CCT245737 | BML-277 | Prexasertib | PD0166285 | CHK1-IN-3 | CHK1-IN-4 hydrochloride | A-443654 | Prexasertib dihydrochloride | BX795 | ANI-7 | Baricitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
