1439399-58-2
CB-839
CAS: 1439399-58-2
Molecular Formula: C26H24F3N7O3S
1439399-58-2 - Names and Identifiers
1439399-58-2 - Physico-chemical Properties
| Molecular Formula | C26H24F3N7O3S |
| Molar Mass | 571.57 |
| Density | 1.430±0.06 g/cm3(Predicted) |
| Melting Point | 186- 189° C |
| Solubility | DMSO: ≥ 30 mg/mL |
| Appearance | Yellow solid |
| Color | Pale yellow |
| pKa | 8.25±0.50(Predicted) |
| Storage Condition | +2C to +8C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
| In vitro study | CB-839 exhibits time-dependent and slowly reversible kinetics. IC50 values for glutaminase inhibition by CB-839 following preincubation with rHu-GAC for-1 hour are < 50 nmol/L, at least 13-fold lower than with BPTES. CB-839 has antiproliferative activity in a triple-negative breast cancer (TNBC) cell line, HCC-1806 while no antiselective activity is observed in an estrogen receptor-positive cell line, T47D. CB-839 exhibits time-dependent and slowly reversible kinetic properties. After preincubation with rHu-GAC for 1 hour, CB-839 inhibited glutaminase with an IC50 value of <50 nmol/L, at least 13-fold lower than that of BPTES. CB-839 has anti-proliferative activity on the triple negative breast cancer (TNBC) cell line, HCC-1806, and no anti-proliferative activity on the estrogen receptor positive cell line, T47D. |
| In vivo study | In the mouse TNBC model, single agent CB-839 (200 mg/kg, p.o.) suppresses tumor growth by 61% relative to vehicle control. In the mouse JIMT-1 xenograft model, CB-839 alone (200 mg/kg, p.o.) results in 54% tumor growth inhibition (TGI) relative to vehicle control, combination of CB-839 (200 mg/kg p.o.) with paclitaxel (10 mg/kg, p.o.) largely sum up the growth of the masses resulting in a TGI relative to vehicle control of 100%. In the mouse TNBC model, a single dose of CB-839 (200 mg/kg, p.o.) tumor growth was inhibited by 61% relative to the vehicle control. In the mouse JIMT-1 xenograft model, CB-839 was administered alone (200 mg/kg, p.o.) resulted in 54% tumor growth inhibition (TGI) relative to vehicle control, CB-839 (200 mg/kg, p.o.) and paclitaxel (10 mg/kg, p.o.) the combination significantly inhibited tumor regrowth, resulting in 100% tumor growth inhibition (TGI) relative to the vehicle control. |
1439399-58-2 - Reference
| Reference Show more | 1. [IF=6.313] Yijia Yang et al."Piperlongumine Inhibits Thioredoxin Reductase 1 by Targeting Selenocysteine Residues and Sensitizes Cancer Cells to Erastin."Antioxidants-Basel. 2022 Apr;11(4):710 |
1439399-58-2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.75 ml | 8.748 ml | 17.496 ml |
| 5 mM | 0.35 ml | 1.75 ml | 3.499 ml |
| 10 mM | 0.175 ml | 0.875 ml | 1.75 ml |
| 5 mM | 0.035 ml | 0.175 ml | 0.35 ml |
Last Update：2024-01-02 23:10:35
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