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EC 144, a second-generation selective inhibitor of Hsp90 (heat shock protein 90), inhibits tumor growth with an IC50= 1.1 nM for Hsp90α and an EC50 = 14 nM for degradation of Her-2 in MCF-7 cells.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 50 mg | $1,980 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks | 6-8 weeks |
| Description | EC 144, a second-generation selective inhibitor of Hsp90 (heat shock protein 90), inhibits tumor growth with an IC50= 1.1 nM for Hsp90α and an EC50 = 14 nM for degradation of Her-2 in MCF-7 cells. |
| In vitro | EC 144 is a synthetic Hsp90 inhibitor, blocks LPS-induced TLR4 signaling in RAW 264.7 cells by inhibiting activation of ERK1/2, MEK1/2, JNK, and p38 MAPK but not NF-κB. EC 144 inhibited CD4(+) T cell proliferation in both mouse and human mixed lymphocyte reactions (MLRs), indicating an immunosuppressive effect on adaptive immune activation. [1] |
| In vivo | In mice treated with EC 144, peritoneal CD11b(+) exudate cells showed reduced phosphorylation of tumor progression locus 2, MEK1/2, and ERK1/2 upon LPS challenge. This corresponded with resistance to LPS-induced systemic inflammation and suppressed TNF-α release. In a mouse collagen-induced arthritis model, EC 144 suppressed arthritis development, correlated with a reduction in antigen-specific antibody production and impaired activation of antigen-specific CD4(+) T cells. [1] |
| Synonyms | EC144 |
| Molecular Weight | 413.9 |
| Formula | C21H24ClN5O2 |
| Cas No. | 911397-80-3 |
| Smiles | ClC1=NC(=NC2=C1C(C#CCC(O)(C)C)=CN2CC3=NC=C(C(OC)=C3C)C)N |
| Relative Density. | 1.29±0.1 g/cm3(20 °C , 760mmHg) |
| Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (120.8 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.83 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
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DMSO
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