Gamcemetinib

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Gamcemetinib

CAS 1887069-10-4

CC-99677 , OS2IR8TV1O

Molecular Weight	469.94
Formula	C₂₂H₂₀ClN₅O₃S

(10R)-3-[[2-Chloro-5-(ethoxymethyl)-4-pyrimidinyl]oxy]-9,10,11,12-tetrahydro-10-methyl-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (ACI)
(10R)-3-{[2-chloro-5-(ethoxymethyl)pyrimidin-4-yl]oxy}-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one
BMS 986371
BMS-986371
CC 99677
CC-99677

(R)-3-((2-Chloro-5-(ethoxymethyl)pyrimidin-4-yl)oxy)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one

OriginatorCelgene Corporation
ClassAnti-inflammatories
Mechanism of ActionMAP-kinase-activated kinase 2 inhibitors
Orphan Drug StatusNo

14 Nov 2024Efficacy and adverse events data from a phase II trial in Ankylosing Spondylitis presented at the ACR Convergence 2024 (ACR-2024)
27 Mar 2024Pharmacokinetics and adverse events data from a phase I trial (In volunteers) presented at the 125^th Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics 2024 (ASCPT-2024)
26 Oct 2023Discontinued – Phase-I for Inflammation (In volunteers) in USA, United Kingdom (PO) prior to October 2023 (Bristol-Myers Squibb pipeline, October 2023)

Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC₅₀=156.3 nM) and cell based assays (EC₅₀=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1.

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