(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide Basic information
- Product Name:
- (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
- Synonyms:
-
- (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
- EOS-62352
- GDC0575 hydrochloride
- GDC0575 monohydrochloride
- GDC0575 monohydrochloride,GDC-0575 monohydrochloride
- GDC0575 monohydrochloride, 10 mM in DMSO
- CAS:
- 1196504-54-7
- MF:
- C16H21BrClN5O
- MW:
- 414.73
- Mol File:
- 1196504-54-7.mol
(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide 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
GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for?colitis-associated cancer (CAC) and colitis research[1].
in vitro
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._x000D_ _x000D_ Reference: Nat Commun. 2017 Nov 22;8(1):1679. https://pubmed.ncbi.nlm.nih.gov/29162833/
in vivo
GDC-0575 dihydrochloride (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. GDC-0575 dihydrochloride elevates the cytotoxicity of AraC in different primary AML models in vivo[1]. GDC-0575 dihydrochloride (25, 50 mg/kg, p.o.) dose-dependently inhibits the growth of tumor in D20 and C002 xenografts[2].
target
GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2?nM.
IC 50
Chk1: 1.2 nM (IC50)
References
[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. DOI:10.1093/annonc/mdy039
[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. DOI:10.1038/s41467-017-01834-4
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