GDC-0575
GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
Product Specifications
CAS Number
1196541-47-5
Product Name Alternative
ARRY-575; RG7741
UNSPSC
12352005
Hazard Statement
H302
Target
Checkpoint Kinase (Chk)
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GDC-0575.html
Concentration
10mM
Purity
99.50
Solubility
DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL
Smiles
O=C(C1CC1)NC2=CNC3=NC=C(Br)C(N4C[C@H](N)CCC4)=C32
Molecular Formula
C16H20BrN5O
Molecular Weight
378.27
Precautions
H302
References & Citations
[1]Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Mar 13. doi: 10.1158/1078-0432.CCR-17-2701.|[2]Laroche-Clary A, et al. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications. Ann Oncol. 2018 Apr 1;29 (4) :1023-1029.|[3]Di Tullio A, et al. The combination of CHK1 inhibitor with G-CSF overrides cytarabine resistance in human acute myeloid leukemia. Nat Commun. 2017 Nov 22;8 (1) :1679.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Citation 01
Mol Cancer Res. 2020 Jan;18 (1) :91-104.|Mol Cancer. 2024 Apr 29;23 (1) :86.|Nat Commun. 2020 Jan 8;11 (1) :123. |Neurotherapeutics. 2022 Mar;19 (2) :570-591.|Research Square Preprint. 2024 Nov 06.|bioRxiv. 2023 Feb 7.
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