EC 144

Product Description

EC 144 is a high affinity, potent and selective Hsp90 inhibitor (K_i = 0.2 nM and IC₅₀ = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (K_i 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.

Solubility

Preparing Stock Solutions for EC 144

The following data is based on the product molecular weight 413.90

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.42 mL	12.08 mL	24.16 mL
5 mM	0.48 mL	2.42 mL	4.83 mL
10 mM	0.24 mL	1.21 mL	2.42 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Yun EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity. J.Immunol. 2011 PMID: 21131419
• Shi EC144 is a potent inhibitor of the heat shock protein 90. J.Med.Chem. 2012 PMID: 22938030