NMS-E973 |
Catalog No.GC13105
One-Click Copy Product Info
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Hsp90 inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1253584-84-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1253584-84-7 | SDF | |
| Canonical SMILES | CN1CCC(CC1)NC(=O)C2=CC(=C3C(=CC(=O)C=C3OC4=CC=C(C=C4)[N+](=O)[O-])O)ON2 | ||
| Formula | C22H22N4O7 | M.Wt | 454.43 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2006 mL | 11.0028 mL | 22.0056 mL |
| 5 mM | 440.1 μL | 2.2006 mL | 4.4011 mL |
| 10 mM | 220.1 μL | 1.1003 mL | 2.2006 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)