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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% (HPLC)
Biological Activity for EC 144
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.
Compound Libraries for EC 144
EC 144 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for EC 144
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for EC 144
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.39 | 100 | |
| ethanol | 2.07 | 5 |
Preparing Stock Solutions for EC 144
The following data is based on the product molecular weight 413.9. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for EC 144
References for EC 144
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for EC 144, please let us know.
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Keywords: EC 144, EC 144 supplier, EC144, high, affinity, potent, selective, HSP90, heat, shock, proteins, inhibitors, inhibits, her-2, antitumor, orally, available, brain, penetrant, Hsp90, 4701, Tocris Bioscience
1 Citation for EC 144
Citations are publications that use Tocris products. Selected citations for EC 144 include:
Catherine B et al (2021) Inhibition of the NLRP3 inflammasome by HSP90 inhibitors. Immunology 162 84-91 PMID: 32954500
Do you know of a great paper that uses EC 144 from Tocris? Please let us know.
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Literature in this Area
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
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