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| | 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Basic information |
| Product Name: | 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide | | Synonyms: | NMS-E973;5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide;3-Isoxazolecarboxamide, 5-[2,4-dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-;5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide USP/EP/BP;NMS-E973,Leukemia,NMS E973,inhibit,HSP,Heat shock proteins,Adenocarcinoma,Hsp90α,ovary,colon,breast,cancer,Carcinoma,Neuroblastoma,NMSE973,NMS-E-973,Melanoma,Inhibitor | | CAS: | 1253584-84-7 | | MF: | C22H22N4O7 | | MW: | 454.43 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1253584-84-7.mol | ![5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Structure](CAS/20180629/GIF/1253584-84-7.gif) |
| | 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Chemical Properties |
| Boiling point | 686.9±55.0 °C(Predicted) | | density | 1.50±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder | | pka | 5.69±0.20(Predicted) |
| | 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Usage And Synthesis |
| Biological Activity | 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]. | | target | Hsp90 | | 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. |
| | 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide Preparation Products And Raw materials |
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