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EC 144

Cat. No. M6697

All AbMole products are for research use only, cannot be used for human consumption.

EC 144 Structure

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Quality Control & Documentation
Biological Activity

EC 144 is a high affinity, potent and selective Hsp90 inhibitor (Ki = 0.2 nM and IC50 = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (Ki values are 61 and 255 nM respectively) and has no effect (IC50 >10 μM) against a panel of 285 kinases. Degrades Her-2 in MCF-7 breast cancer cells (EC50 = 14 nM). Blocks tumor growth and induces partial tumor regression in an N87 gastric tumor mouse model. Also inhibits LPS-induced TNFα release in an LPS shock mouse model and suppresses disease development in a rat model of collagen-induced arthritis. Exhibits <20-fold efficacy over BIIB 021 in mice. Orally available and brain penetrant.

Chemical Information
Molecular Weight 413.9
Formula C21H24ClN5O2
CAS Number 911397-80-3
Solubility (25°C) DMSO 41.39 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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Abmole Inhibitor Catalog




Keywords: EC 144 supplier, inhibitors, activators

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