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R&D Systems™ EC 144
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Catalog No. 470110 Shop All Novus Products
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47-011-0 10 mg
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Catalog No. 47-011-0 Supplier R&D Systems™ Supplier No. 4701/10

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Description

A Tocris product, part of R&D Systems. High affinity, potent and selective Hsp90 inhibitor

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 (Cat. No. 4608) in mice. Orally available and brain penetrant.

Specifications

Quantity 10 mg
Product Line Tocris
Product Type EC 144
Purity >98%
Molecular Weight (g/mol) 413.9
Inhibitors EC 144

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