(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide

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Products Intro: Product Name:GDC0575 hydrochloride
CAS:1196504-54-7
Purity:98% Package:10MG;50MG;100MG,1G,5G,10G.100G
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Products Intro: Product Name:GDC0575 monohydrochloride；GDC0575;ARRY-575;GDC-0575;GDC 0575;ARRY575
CAS:1196504-54-7
Package:10 mg；100 mg；2 mg；25 mg；5 mg；50 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
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CAS:1196504-54-7
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Products Intro: Product Name:GDC0575 hydrochloride
CAS:1196504-54-7
Purity:98% HPLC LCMS Package:100mg;500mg;1g;5g;10g
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Products Intro: Product Name:EOS-62352
CAS:1196504-54-7
Purity:99% HPLC Package:5KG;1KG
(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;(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide hydrochloride
CAS:1196504-54-7
MF:C16H21BrClN5O
MW:414.73
EINECS:
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Mol File:1196504-54-7.mol
(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide Structure
(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide Chemical Properties
Safety Information
MSDS Information
(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide Usage And Synthesis
DescriptionGDC-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 1.2nM. 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.
UsesGDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used forcolitis-associated cancer (CAC) and colitis research[1].
in vitroCHK1 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].

targetGDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2nM.
IC 50Chk1: 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
(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide Preparation Products And Raw materials
Tag:(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide(1196504-54-7) Related Product Information
giredestrant (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide GDC0575 2,6-dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide GDC-0077 (S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one XL518 DONEPEZIL HYDROCHLORIDE