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NMS-E973

SKU: orb1685642

Description

NMS-E973

Research Area

Metabolism Research, Signal Transduction

Images & Validation

Key Properties

CAS Number1253584-84-7
MW454.43
Purity99.84%
FormulaC22H22N4O7
SMILESCN1CCC(CC1)NC(=O)c1cc(on1)-c1c(O)cc(O)cc1Oc1ccc(cc1)[N+]([O-])=O
TargetHSP
SolubilityDMSO: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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor 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
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Key Properties

No computed properties available.

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NMS-E973 (orb1685642)

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Step 2: Enter the in vivo formulation

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
$ 80.00
5 mg
$ 100.00
1 ml x 10 mM (in DMSO)
$ 110.00
10 mg
$ 140.00
25 mg
$ 250.00
50 mg
$ 370.00
100 mg
$ 510.00
200 mg
$ 700.00
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