[CAS NO. 1253584-84-7] NMS-E973
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PRODUCTS SPECIFICATIONS [1253584-84-7]
Catalog
SLK-S7282
Brand
Selleck
CAS
1253584-84-7
DESCRIPTION [1253584-84-7]
Overview
| MDL | MFCD28099810 |
|---|---|
| Molecular Weight | 454.43 |
| Molecular Formula | C22H22N4O7 |
| SMILES | O=C(C1=NOC(C2=C(OC3=CC=C([N+]([O-])=O)C=C3)C=C(O)C=C2O)=C1)NC4CCN(C)CC4 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2006 mL | 11.0028 mL | 22.0056 mL |
| 5 mM | 0.4401 mL | 2.2006 mL | 4.4011 mL |
| 10 mM | 0.2201 mL | 1.1003 mL | 2.2006 mL |
| 50 mM | 0.0440 mL | 0.2201 mL | 0.4401 mL |
Description
NMS-E973 is a potent and selective inhibitor with of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.
Targets
| HSP90 [1] |
| <10 nM(DC50) |
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.
References
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