NMS-E973

SKU: orb1685642

Description

NMS-E973

Research Area

Metabolism Research, Neuroscience, Signal Transduction

Key Properties

• CAS Number: 1253584-84-7
• MW: 454.43
• Purity: 99.84% (May vary between batches)
• Formula: C₂₂H₂₂N₄O₇
• SMILES: CN1CCC(CC1)NC(=O)c1cc(on1)-c1c(O)cc(O)cc1Oc1ccc(cc1)[N+]([O-])=O
• Target: HSP
• Solubility: DMSO:83 mg/mL (182.65 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.26 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HSP90:<10 nM(DC50)
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

colon, breast, Carcinoma, Adenocarcinoma, cancer, Melanoma, Leukemia, Heat shock proteins, Inhibitor, Hsp90α, HSP90, HSP, inhibit, NMS E973, NMS-E 973, NMSE973, NMS-E973, NMS-E-973, ovary, Neuroblastoma

Compound Identifiers

PubChem CID

135566652