Dual DDR1 and DDR2 inhibitor 5n|

Cas No.:	2241813-33-0
Chemical Name:	3-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide
Synonyms:	3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide;3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-~{N}-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-propan-2-yl-benzamide;Dual DDR1 and DDR2 inhibitor 5n;DDR1/2 inhibitor 5n;GTPL10105;TQP0794;BDBM50368452;3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-propan-2-ylbenzamide;FEW;N-;2241813-33-0;2241813-33-0;CHEMBL4168305;CHEMBL4168305;N-(3-(trifluoromethyl)-5-((4-methylpiperazin-1-yl)methyl)phenyl)-3-(2-(imidazo[1,2-a]pyrazin-3-yl)ethynyl)-4-isopropylbenzamide;N-(3-(trifluoromethyl)-5-((4-methylpiperazin-1-yl)methyl)phenyl)-3-(2-(imidazo[1,2-a]pyrazin-3-yl)ethynyl)-4-isopropylbenzamide;starbld0048679;starbld0048679
SMILES:	FC(C1C=C(C=C(C=1)CN1CCN(C)CC1)NC(C1C=CC(=C(C#CC2=CN=C3C=NC=CN23)C=1)C(C)C)=O)(F)F
Formula:	C₃₁H₃₁F₃N₆O
M.Wt:	560.612656831741
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Dual DDR1 and DDR2 inhibitor 5n is a highly potent, selective, dual Discoidin domain receptor DDR1 and DDR2 inhibitor with Kd of 7.9 and 8.0 nM, IC50 of 9.4 and 20.4 nM, repectively; displays significant selectivity against a panel of 403 wild-type kinases at 1 uM (Abl1 IC50=494 nM); dose-dependently inhibited lipopolysaccharide (LPS)-induced interleukin-6 (IL-6) release in mouse primary peritoneal macrophages (MPMs), attenuates lung pathophysiologic changes in LPS-challenged mice, effectively decreases the levels of TNF-α and IL-6 both in BALF and serum.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC11175	Dual DDR1 and DDR2 inhibitor 5n	Dual DDR1 and DDR2 inhibitor 5n is a highly potent and selective small molecule inhibitor targeting both Discoidin Domain Receptor 1 (DDR1) and Discoidin Domain Receptor 2 (DDR2). These receptors are receptor tyrosine kinases (RTKs) that play critical roles in cell proliferation, migration, and extracellular matrix (ECM) remodeling. Dysregulation of DDR1 and DDR2 has been implicated in various diseases, including cancer, fibrosis, and inflammation, making them attractive therapeutic targets.
DC10996	DDR inhibitor X	DDR inhibitor X is a potent discoidin domain receptor (DDR) inhibitor with IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM..