[CAS NO. 526-18-1] Osalmid
PRODUCTS SPECIFICATIONS [526-18-1]
DESCRIPTION [526-18-1]
Overview
| MDL | MFCD00020026 |
|---|---|
| Molecular Weight | 229.23 |
| Molecular Formula | C13H11NO3 |
| SMILES | O=C(NC1=CC=C(O)C=C1)C2=CC=CC=C2O |
Summary
Osalmid is a ribonucleotide reductase small subunit M2 ( RRM2 ) targeting compound; suppresses ribonucleotide reductase activity with an IC 50 of 8.23 μM.
IC50 & Target
IC50: 8.23 μM (ribonucleotide reductase) [1]
In Vitro
Osalmid is identified as a potential ribonucleotide reductase small subunit M2 (RRM2) compound. Osalmid is 10-fold more active in inhibiting ribonucleotide reductase (RR) activity than hydroxyurea, and significantly inhibits HBV DNA and cccDNA synthesis in HepG2.2.15 cells in a time- and dose-dependent manner. After treatment for 8 days with Osalmid, the EC 50 for HBV DNA inhibition are 11.1 μM for culture supernatant and 16.5 μM for cells. Osalmid suppresses RR activity in a concentration-dependent manner, with an IC 50 of 8.23 μM. Osalmid is shown to possess potent activity against a 3TC-resistant HBV strain, suggesting utility in treating drug-resistant HBV infections [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Osalmid reduces RR activity and HBV replication in HBV-transgenic mice and shows a synergistic efficacy with 3TC without significant toxicity. Oral dosing of osalmid at 400 mg/kg/d results in a time-dependent inhibition of HBV DNA replication. After treatment for 4 weeks, osalmid suppresses HBV DNA replication by about 40-45% as compared to the control in mouse sera and liver tissues [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03670173 | Shanghai 10th People´s Hospital|Shanghai Institute of Materia Medica, Chinese Academy of Sciences |
Multiple Myeloma
|
October 1, 2018 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 436.24 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.3624 mL | 21.8122 mL | 43.6243 mL |
| 5 mM | 0.8725 mL | 4.3624 mL | 8.7249 mL |
| 10 mM | 0.4362 mL | 2.1812 mL | 4.3624 mL |
Synonyms