EOS-62353
EOS-62353 Basic information
- Product Name:
- EOS-62353
- Synonyms:
-
- EOS-62353
- GDC-0575 dihydrochloride
- GDC-0575 2HCl
- CAS:
- 1657014-42-0
- MF:
- C16H21BrClN5O
- MW:
- 414.73
- Mol File:
- 1657014-42-0.mol
EOS-62353 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : 65 mg/mL (144.06 mM)
- form
- Solid
- color
- Light yellow to yellow
EOS-62353 Usage And Synthesis
Description
GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2?nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.
Uses
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
in vivo
GDC-0575 (7.5 mg/kg, p.o.) in combination with AraC alomost completely eradicates leukemic burden in mice transplanted with U937-Luc cells, and shows more efficient activity than AraC alone. Furthermore, GDC-0575 elevates the cytotoxicity of AraC in different primary AML models in vivo[1]. GDC-0575 (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts[2].
IC 50
Chk1: 1.2 nM (IC50)
References
[1] 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. DOI:10.1038/s41467-017-01834-4
[2] Oo ZY, et al. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Jun 15;24(12):2901-2912. DOI:10.1158/1078-0432.CCR-17-2701
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