Dual DDR1 and DDR2 inhibitor 5n( —— )

Catalog No. M13594 CAS No. 2241813-33-0

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Product Name

Dual DDR1 and DDR2 inhibitor 5n
Note

Research use only, not for human use.
Brief 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.
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.
In Vitro

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In Vivo

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Synonyms

——
Pathway

Tyrosine Kinase
Target

DDR
Recptor

DDR
Research Area

——
Indication

——

CAS Number

2241813-33-0
Formula Weight

560.625
Molecular Formula

C31H31F3N6O
Purity

>98% (HPLC)
Solubility

——
SMILES

CC(C)C1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)CN3CCN(CC3)C)C#CC4=CN=C5N4C=CN=C5
Chemical Name

3-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide

1. Wang Z, et al. J Med Chem. 2018 Aug 3. doi: 10.1021/acs.jmedchem.8b01045.

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