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GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $51 | In Stock | |
5 mg | $116 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $432 | In Stock | |
50 mg | $639 | In Stock | |
100 mg | $890 | In Stock | |
1 mL x 10 mM (in DMSO) | $127 | In Stock |
Description | GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM). |
Targets&IC50 | Chk1:1.2 nM |
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]. |
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]. |
Alias | RG7741, ARRY-575 |
Molecular Weight | 378.27 |
Formula | C16H20BrN5O |
Cas No. | 1196541-47-5 |
Smiles | N[C@@H]1CCCN(C1)c1c(Br)cnc2[nH]cc(NC(=O)C3CC3)c12 |
Relative Density. | 1.619 g/cm3 (Predicted) |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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