EC 144

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EC 144 | CAS No. 911397-80-3 | HSP90 Inhibitors
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Description: High affinity, potent and selective Hsp90 inhibitor

Chemical Name: 5-[2-Amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2-methyl-4-pentyn-2-ol

Purity: ≥98%

Product Details
Citations (1)
Reviews

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

Technical Data

M.Wt:
413.9
Formula:
C21H24ClN5O2
Solubility:
Soluble to 100 mM in DMSO and to 5 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
911397-80-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citation for EC 144

The citations listed below are publications that use Tocris products. Selected citations for EC 144 include:

1 Citation: Showing 1 - 1

  1. Inhibition of the NLRP3 inflammasome by HSP90 inhibitors.
    Authors: Catherine B Et al.
    Immunology  2021;162:84-91

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