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[CAS NO. 56990-57-9] NSC-87877
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18756 |
| Brand: | MCE |
| CAS: | 56990-57-9 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 459.45 |
| Molecular Formula | C19H13N3O7S2 |
| SMILES | O=S(C1=C2C=CC=NC2=C(O)C(/N=N/C3=CC=C4C=C(S(=O)(O)=O)C=CC4=C3)=C1)(O)=O |
Summary
NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC 50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively [1] . NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26) [2] .
IC50 & Target
IC50: 0.318 μM (shp2), 0.355 μM (shp1) [1] .
In Vitro
NSC-87877 (0-0.5 μM, 5 days) inhibits DUSP26 function in NB cell lines
[3]
.
NSC-87877 (0-0.5 μM, 5 days) results in increased p53 phosphorylation (Ser37 and Ser46) and activation
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
| Cell Line: | p53 wild-type neuroblastoma (NB) cell lines [2] . |
| Concentration: | 0, 0.25, 0.5 μM. |
| Incubation Time: | 5 dsys. |
| Result: |
Resulted in increased p53 phosphorylation (Ser37 and Ser46) and activation, increased activation of downstream p38 effector proteins (heat shock protein 27 (HSP27) and MAP kinase-activated protein kinase 2 (MAPKAPK2)) and poly ADP ribose polymerase/caspase-3 cleavage.
Inhibited DUSP26 function in NB cell lines. Resulted in apoptosis in many cell lines at varying IC 50 levels of 1.84 μM (IMR32), 6.35 μM (SK-N-SH), 8.69 μM (NB-19), 12.6 μM (SMS-KCN), 15.7 μM (SH-SY5Y), 15.8 μM (JF) and 19.0 μM (CHLA-225), respectively. |
In Vivo
NSC-87877 (30 mg/kg, IP once daily for 15 days) possesses excellent anti- neuroblastoma activity
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Intrarenal neuroblastoma (NB) tumor mouse model in female nude mice
[3]
.
|
| Dosage: | 30 mg/kg. |
| Administration: | IP once daily for 15 days. |
| Result: | Significantly inhibited NB tumor growth. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 23.81 mg/mL ( 51.82 mM ; ultrasonic and warming and heat to 60°C)
DMSO : 20 mg/mL ( 43.53 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1765 mL | 10.8826 mL | 21.7652 mL |
| 5 mM | 0.4353 mL | 2.1765 mL | 4.3530 mL |
| 10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 3.33 mg/mL (7.25 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution
References
- [1] Chen L, et al. Discovery of a novel shp2 protein tyrosine phosphatase inhibitor. Mol Pharmacol. 2006 Aug;70(2):562-70.
- [2] Song M, et al. NSC-87877, inhibitor of SHP-1/2 PTPs, inhibits dual-specificity phosphatase 26 (DUSP26). Biochem Biophys Res Commun. 2009 Apr 17;381(4):491-5.
- [3] Y Shi, et al. NSC-87877 inhibits DUSP26 function in neuroblastoma resulting in p53-mediated apoptosis. Cell Death Dis. 2015 Aug 6;6(8):e1841.
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