EC 144

   
Product Datasheet
Catalog Number:4701
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
Product Details
Reviews
Biological Activity
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
  • 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. All Tocris products are intended for laboratory research use only.
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