[CAS NO. 2170606-74-1] DB2313
PRODUCTS SPECIFICATIONS [2170606-74-1]
DESCRIPTION [2170606-74-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 708.83 |
| Molecular Formula | C42H41FN8O2 |
| SMILES | FC1=C(COC2=CC=C(C3=NC4=CC=C(C(NC(C)C)=N)C=C4N3)C=C2)C=CC=C1COC5=CC=C(C6=NC7=CC=C(C(NC(C)C)=N)C=C7N6)C=C5 |
Summary
IC50 & Target
IC50: 14 nM (PU.1) [1]
In Vitro
DB2313 treatment leads to a profound decrease in the growth of PU.1 URE
–/–
acute myeloid leukemia (AML) cells (IC
50
of 7.1 μM), while showing little effect on normal hematopoietic cells at similar concentrations. DB2313 treatment leads to a 3.5-fold increase in apoptotic cells in murine PU.1 URE
–/–
AML cells. DB2313 also leads to a significant decrease in clonogenicity in the second and third rounds of plating and a complete disruption of clonogenic capacity in the fourth and higher rounds of plating
[1]
.
In AML cells, DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
DB2313 (17 mg/kg; i.p.; three times per week; for 3 weeks) treatment decreases leukemia progression and results in increased survival in mice [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | NSG mice bearing sublethally irradiated (2.0 Gy) and injection with PU.1 URE –/– AML cells [1] |
| Dosage: | 17 mg/kg |
| Administration: | Intraperitoneal injection; three times per week; for 3 weeks |
| Result: | Decreased tumor burden and resulted in increased survival. |
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 : 3.7 mg/mL ( 5.22 mM ; ultrasonic and warming and heat to 70°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4108 mL | 7.0539 mL | 14.1078 mL |
| 5 mM | 0.2822 mL | 1.4108 mL | 2.8216 mL |
| 10 mM | --- | --- | --- |
-
1.
Add each solvent one by one: 50% PEG300 >> 50% saline
Solubility: 5 mg/mL (7.05 mM); Suspended solution; Need ultrasonic
References
- [1] Iléana Antony-Debré, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313.
- [2] Zhang S, Zhao S, Qi Y, et al. SPI1-induced downregulation of FTO promotes GBM progression by regulating pri-miR-10a processing in an m6A-dependent manner. Mol Ther Nucleic Acids. 2022;27:699-717.
