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NMS-E973

Hsp90 inhibitor,potent and selective CAS# 1253584-84-7

NMS-E973

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Chemical structure

NMS-E973

3D structure

Chemical Properties of NMS-E973

Cas No. 1253584-84-7 SDF Download SDF
PubChem ID 71463575 Appearance Powder
Formula C22H22N4O7 M.Wt 454.43
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name (5E)-5-[2-hydroxy-6-(4-nitrophenoxy)-4-oxocyclohexa-2,5-dien-1-ylidene]-N-(1-methylpiperidin-4-yl)-2H-1,2-oxazole-3-carboxamide
SMILES CN1CCC(CC1)NC(=O)C2=CC(=C3C(=CC(=O)C=C3OC4=CC=C(C=C4)[N+](=O)[O-])O)ON2
Standard InChIKey LNOSECQICJNHTG-QZQOTICOSA-N
Standard InChI InChI=1S/C22H22N4O7/c1-25-8-6-13(7-9-25)23-22(29)17-12-20(33-24-17)21-18(28)10-15(27)11-19(21)32-16-4-2-14(3-5-16)26(30)31/h2-5,10-13,24,28H,6-9H2,1H3,(H,23,29)/b21-20+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of NMS-E973

DescriptionNMS-E973 is a potent and selective inhibitor of Hsp90.
TargetsHsp90    

NMS-E973 Dilution Calculator

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Preparing Stock Solutions of NMS-E973

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2006 mL 11.0028 mL 22.0056 mL 44.0112 mL 55.014 mL
5 mM 0.4401 mL 2.2006 mL 4.4011 mL 8.8022 mL 11.0028 mL
10 mM 0.2201 mL 1.1003 mL 2.2006 mL 4.4011 mL 5.5014 mL
50 mM 0.044 mL 0.2201 mL 0.4401 mL 0.8802 mL 1.1003 mL
100 mM 0.022 mL 0.11 mL 0.2201 mL 0.4401 mL 0.5501 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on NMS-E973

NMS-E973 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with DC50 value of < 10nM [1].

Since Hsp90 plays an important role in the conformational maturation, stability and function of some oncogenic proteins, the inhibitors of Hsp90 are developed as therapeutic for cancers. NMS-E973 is a selective inhibitor of Hsp90. It binds to Hsp90α within the ATP binding site with DC50 value of < 10nM. Besides that, NMS-E973 shows no effect on a panel of 52 various protein kinases such as ABL, ACK1, AKT1 and Alk. The IC50 value of it for Hsc70 is > 10μM. NMS-E973 exerts antiproliferation effects on A2780 tumor cell line and BT-474 breast cancer cell line with IC50 values of 69nM and 110nM, respectively. When treated with mice bearing A2780 xenografts, the intravenous administration of NMS-E973 significantly inhibits tumor growth with TGI value of 53% at dose of 30mg/kg. Moreover, NMS-E973 also displays antitumor activity in tumors resistant to kinase inhibitors such as vemurafenib [1, 2].

References:
[1] Brasca M G, Mantegani S, Amboldi N, et al. Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). Bioorganic & medicinal chemistry, 2013, 21(22): 7047-7063.
[2] Fogliatto G, Gianellini L, Brasca M G, et al. NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases. Clinical Cancer Research, 2013, 19(13): 3520-3532.

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References on NMS-E973

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).[Pubmed:24100158]

Bioorg Med Chem. 2013 Nov 15;21(22):7047-63.

Novel small molecule inhibitors of heat shock protein 90 (Hsp90) were discovered with the help of a fragment based drug discovery approach (FBDD) and subsequent optimization with a combination of structure guided design, parallel synthesis and application of medicinal chemistry principles. These efforts led to the identification of compound 18 (NMS-E973), which displayed significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile.

NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.[Pubmed:23674492]

Clin Cancer Res. 2013 Jul 1;19(13):3520-32.

PURPOSE: Recent developments of second generation Hsp90 inhibitors suggested a potential for development of this class of molecules also in tumors that have become resistant to molecular targeted agents. Disease progression is often due to brain metastases, sometimes related to insufficient drug concentrations within the brain. Our objective was to identify and characterize a novel inhibitor of Hsp90 able to cross the blood-brain barrier (BBB). EXPERIMENTAL DESIGN: Here is described a detailed biochemical and crystallographic characterization of NMS-E973. Mechanism-based anticancer activity was described in cell models, including models of resistance to kinase inhibitors. Pharmacokinetics properties were followed in plasma, tumor, liver, and brain. In vivo activity and pharmacodynamics, as well as the pharmacokinetic/pharmacodynamic relationships, were evaluated in xenografts, including an intracranially implanted melanoma model. RESULTS: NMS-E973, representative of a novel isoxazole-derived class of Hsp90 inhibitors, binds Hsp90alpha with subnanomolar affinity and high selectivity towards kinases, as well as other ATPases. It possesses potent antiproliferative activity against tumor cell lines and a favorable pharmacokinetic profile, with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 induces tumor shrinkage in different human tumor xenografts, and is highly active in models of resistance to kinase inhibitors. Moreover, consistent with its brain penetration, NMS-E973 is active also in an intracranially implanted melanoma model. CONCLUSIONS: Overall, the efficacy profile of NMS-E973 suggests a potential for development in different clinical settings, including tumors that have become resistant to molecular targeted agents, particularly in cases of tumors which reside beyond the BBB.

Description

NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.

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