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EC144

Chemical Structure : EC144

CAS No.: 911397-80-3

EC144 (EC-144)

Catalog No.: PC-21226Not For Human Use, Lab Use Only.

EC144 (EC-144) is a potent, second generation inhibitor of heat shock protein 90 (Hsp90) with IC50 of 1.1 nM in Hsp90α binding assay, degrades Her-2 in MCF-7 cells with EC50 of 14 nM.

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Biological Activity

EC144 (EC-144) is a potent, second generation inhibitor of heat shock protein 90 (Hsp90) with IC50 of 1.1 nM in Hsp90α binding assay, degrades Her-2 in MCF-7 cells with EC50 of 14 nM.
EC144 inhibits tumor growth at 5 mg/kg and causes partial tumor regressions at 10 mg/kg (po, qd × 5) in mouse model of gastric tumors (N87).
EC144 is approximately 20-fold more efficacious than BIIB021 (Cat# PC-42459).
EC144 blocks LPS-induced TLR4 signaling in RAW 264.7 cells by inhibiting activation of ERK1/2, MEK1/2, JNK, and p38 MAPK but not NF-κB.
EC144 blocks disease development in rat collagen-induced arthritis by suppressing the inflammatory response.

Physicochemical Properties

M.Wt 413.91
Formula C21H24ClN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol

References

1. Shi J, et al. J Med Chem. 2012 Sep 13;55(17):7786-95.

2. Yun TJ, et al. J Immunol. 2011 Jan 1;186(1):563-75.

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