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

Product Name: (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
CAS No.: 1196504-54-7
Chemical Name: (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
Synonyms: EOS-62352;GDC0575 hydrochloride;GDC0575 monohydrochloride;GDC0575 monohydrochloride, 10 mM in DMSO;GDC0575 monohydrochloride,GDC-0575 monohydrochloride;(R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamide
CBNumber: CB53142373
Molecular Formula: C16H21BrClN5O
Formula Weight: 414.73
MOL File: 1196504-54-7.mol

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Biosynth Carbosynth

Product number: FG172882
Product name: GDC 0575 hydrochloride
Packaging: 50mg
Price: $1100
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FG172882
Product name: GDC 0575 hydrochloride
Packaging: 100mg
Price: $1350
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FG172882
Product name: GDC 0575 hydrochloride
Packaging: 250mg
Price: $2400
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FG172882
Product name: GDC 0575 hydrochloride
Packaging: 500mg
Price: $2850
Updated: 2021/12/16

AK Scientific

Product number: 2505DT
Product name: GDC0575hydrochloride
Packaging: 500mg
Price: $3897
Updated: 2021/12/16

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

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

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

Raw materials

Preparation Products

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

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1196504-54-7, (R)-N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)cyclopropanecarboxamideRelated Search:

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

(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

1196504-54-7