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GDC-0575

Catalog No. T7300 CAS 1196541-47-5

Synonyms: ARRY-575, RG7741

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GDC-0575, CAS 1196541-47-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
5 mg	In stock	$ 116.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 432.00
50 mg	In stock	$ 639.00
100 mg	In stock	$ 890.00
1 mL * 10 mM (in DMSO)	In stock	$ 127.00

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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 is significantly more potent in promoting DNA damage, replication stress and cell death than 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].

Synonyms	ARRY-575, RG7741
Molecular Weight	378.27
Formula	C16H20BrN5O
CAS No.	1196541-47-5

Storage

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

Solubility Information

DMSO: 50 mg/mL (132.18 mM)

References and Literature

1. Oo Z Y , Stevenson A J , Proctor M A , et al. Endogenous replication stress marks melanomas sensitive to CHK1 inhibitors in vivo[J]. Clinical Cancer Research, 2018:clincanres.2701.2017. 2. Tullio A D , Rouault-Pierre K , Abarrategi A , et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia[J]. Nature Communications, 2017, 8(1):1679.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library NO PAINS Compound Library Kinase Inhibitor Library Clinical Compound Library Cell Cycle Compound Library

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GDC-0575 1196541-47-5 Cell Cycle/Checkpoint Chk RG 7741 RG-7741 GDC0575 ARRY-575 ARRY575 inhibit Inhibitor Checkpoint Kinase (Chk) ARRY 575 RG7741 GDC 0575 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.