EC 144

Name: EC 144
Brand: Tocris Bioscience
SKU: 4701

Tocris Bioscience, part of Bio-Techne | Catalog # 4701

Citations (2)

COA / SDS

High affinity, potent and selective Hsp90 inhibitor

Key Product Details

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)
Molecular Weight:	413.9

View Full Technical Details for EC 144

Technical Data
Citations

Biological Activity for EC 144

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.

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 for EC 144

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	2.07	5
	DMSO	41.39	100

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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References for EC 144

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