[CAS NO. 2242480-48-2] VPC-18005
PRODUCTS SPECIFICATIONS [2242480-48-2]
DESCRIPTION [2242480-48-2]
Overview
| MDL | MFCD28248832 |
|---|---|
| Molecular Weight | 319.38 |
| Molecular Formula | C15H17N3O3S |
| SMILES | O=C(O)CC(S/C(N1)=N\N=C/C2=CC=C(C(C)C)C=C2)C1=O |
Summary
VPC-18005 inhibits ERG-induced transcription and interacts directly with the
ERG-ETS domain
, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity
[1]
.
In Vitro
VPC-18005 is found to inhibit pETS-luc reporter activity in PNT1B-ERG and VCaP cells with IC
50
values of 3 and 6 μM, respectively
[1]
.
VPC-18005 could suppress ERG reporter activity without exhibiting overt cytotoxicity
[1]
.
VPC-18005 inhibits migration and invasion of ERG-overexpressing cells in vitro
[1]
.
VPC-18005 can antagonize the metastatic potential of ERG-expressing prostate cells
[1]
.
The exposure of larvae to 1 or 10 µM of VPC-18005 produced a 20–30% decrease in the dissemination of cancer cells in zebrafsh
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | PNT1B-Mock cells and PNT1B-ERG cells. |
| Concentration: | 5 µM. |
| Incubation Time: | 24 h. |
| Result: | Inhibited migration and invasion of prostate cell lines in vitro. |
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 : 62.5 mg/mL ( 195.69 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1311 mL | 15.6553 mL | 31.3107 mL |
| 5 mM | 0.6262 mL | 3.1311 mL | 6.2621 mL |
| 10 mM | 0.3131 mL | 1.5655 mL | 3.1311 mL |
References
- [1] Miriam S Butler, et al. Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer. Oncotarget. 2017 Jun 27;8(26):42438-42454.
- [2] Haneen Amawi, et al. The use of zebrafish model in prostate cancer therapeutic development and discovery. Cancer Chemother Pharmacol. 2021 Mar;87(3):311-325.