EC 144

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Cat.No. 4701 - EC 144 | CAS No. 911397-80-3
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% (HPLC)
Datasheet
Citations
Literature

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.

Compound Libraries

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Technical Data

M. Wt 413.9
Formula C21H24ClN5O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 911397-80-3
PubChem ID 11517212
InChI Key VOASEWXFCTZRDF-UHFFFAOYSA-N
Smiles ClC1=C2C(N(CC3=C(C)C(OC)=C(C)C=N3)C=C2C#CCC(C)(C)O)=NC(N)=N1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.39 100

Preparing Stock Solutions

The following data is based on the product molecular weight 413.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Shi et al (2012) EC144 is a potent inhibitor of the heat shock protein 90. J.Med.Chem. 55 7786 PMID: 22938030

Yun et al (2011) EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity. J.Immunol. 186 563 PMID: 21131419


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Keywords: EC144 high affinity potent selective HSP90 heat shock proteins inhibitors inhibits her-2 antitumor orally available brain penetrant Hsp90

Citations for EC 144

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