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GDC-0575

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Catalog No. T7300Cas No. 1196541-47-5
Alias RG7741, ARRY-575

GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).

GDC-0575

GDC-0575

🥰Excellent
Catalog No. T7300Alias RG7741, ARRY-575Cas No. 1196541-47-5
GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).
Pack SizePriceAvailabilityQuantity
1 mg$51In Stock
5 mg$116In Stock
10 mg$197In Stock
25 mg$432In Stock
50 mg$639In Stock
100 mg$890In Stock
1 mL x 10 mM (in DMSO)$127In Stock
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Purity:≥95%
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Product Introduction

Bioactivity
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].
AliasRG7741, ARRY-575
Chemical Properties
Molecular Weight378.27
FormulaC16H20BrN5O
Cas No.1196541-47-5
SmilesN[C@@H]1CCCN(C1)c1c(Br)cnc2[nH]cc(NC(=O)C3CC3)c12
Relative Density.1.619 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.6436 mL13.2181 mL26.4361 mL132.1807 mL
5 mM0.5287 mL2.6436 mL5.2872 mL26.4361 mL
10 mM0.2644 mL1.3218 mL2.6436 mL13.2181 mL
20 mM0.1322 mL0.6609 mL1.3218 mL6.6090 mL
50 mM0.0529 mL0.2644 mL0.5287 mL2.6436 mL
100 mM0.0264 mL0.1322 mL0.2644 mL1.3218 mL

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