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NMS-E973

CAS number:1253584-84-7    molecular formula:C22H22N4O7

overview

compound introduction

Information NMS-E973 NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of Targets HSP90 In vitro NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways. In vivo NMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90. Cell Research(from reference) Cell lines:140 human tumor cell lines of various tissue origins and molecular background. Concentrations:~10 μM

Specs

Chinese alias-
English aliasBCP29502 | NCGC00386326-01 | AKOS027307871 | MS-28264 | A908739 | PD156195 | 5-[2,4-Dihydroxy-6-(4-nitrophenoxy)phenyl]-N-(1-methyl-4-piperidinyl)-3-isoxazolecarboxamide | EX-A4406 | Q27457049 | NMSE973; NMS E973 | SW220107-1 | PD118025 | 5-[2,4-Dihydroxy
CAS number1253584-84-7molecular formulaC22H22N4O7
molecular weight454.43 g/molExact mass10mM in DMSO
PSA154.000 Ųlogp2.811

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