[CAS NO. 2469975-55-9] Nur77modulator1
PRODUCTS SPECIFICATIONS [2469975-55-9]
DESCRIPTION [2469975-55-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 495.60 |
| Molecular Formula | C28H25N5O2S |
| SMILES | CC1=NC2=C(OC)C=CC=C2C(NC3=CC4=C(NC(C(N/N=C/C5=CC=C(SC)C=C5)=O)=C4)C=C3)=C1 |
Summary
IC50 & Target
KD: 3.58 μM (Nur77) [1] .
In Vitro
Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line)
[1]
.
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner
[1]
.
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis
[1]
.
Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1] .
| Cell Line: | Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). |
| Concentration: | 0-20 μM. |
| Incubation Time: | 12-24 hours. |
| Result: |
Exhibited IC
50
values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively.
Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number. |
In Vivo
Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Nude mouse hepatoma HepG2 xenograft [1] . |
| Dosage: | 10 and 20 mg/kg/day. |
| Administration: | IP, once every day for 15 days. |
| Result: |
Lead to substantial suppression of tumor growth.
The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL ( 252.22 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0178 mL | 10.0888 mL | 20.1776 mL |
| 5 mM | 0.4036 mL | 2.0178 mL | 4.0355 mL |
| 10 mM | 0.2018 mL | 1.0089 mL | 2.0178 mL |