[CAS NO. 1630760-75-6] BRD9500
PRODUCTS SPECIFICATIONS [1630760-75-6]
DESCRIPTION [1630760-75-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 291.32 |
| Molecular Formula | C15H18FN3O2 |
| SMILES | O=C1C[C@@H](C)C(C2=CC=C(N3CCOCC3)C(F)=C2)=NN1 |
Summary
IC50 & Target
|
PDE3A 10 nM (IC 50 ) |
PDE3B 27 nM (IC 50 ) |
In Vitro
BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12
[1]
.
BRD9500 exhibits an
EC
50
of 1 nM for SK-MEL-3 melanoma cell line viability
[1]
.
BRD9500 exhibits an
EC
50
of 1.6 nM for HeLa viability
[1]
.
BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | HeLa cells |
| Concentration: | 10 μM |
| Incubation Time: | 8 hours |
| Result: | SLFN12 coimmunoprecipitation was analyzed by immunoblotting with an anti-V5 antibody to detect the SLFN12-V5 fusion protein. The SLFN12-V5 was clearly detected with the anti-V5 antibody. |
In Vivo
BRD9500 (10, 20, and 50 mg/kg; orally) inhibits SK-MEL-3 melanoma growth in mice
[1]
.
BRD9500 shows high plasma levels in mice after iv (1 mg/kg) as well as po (2 mg/kg) dosing over eight hours making it a valuable candidate for in vivo xenograft testing
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female NMRI nude mice bearing SK-MEL-3 melanoma cells tumor xenografts [1] |
| Dosage: | 10, 20, and 50 mg/kg |
| Administration: | Orally at 10 and 20 mg/kg twice daily (2QD) and at 50 mg/kg once per day (QD). |
| Result: | Achieved the strongest antitumor activity at 50 mg/kg. All treatments were well tolerated without critical body weight loss or toxicities. |
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 : 50 mg/mL ( 171.63 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.4327 mL | 17.1633 mL | 34.3265 mL |
| 5 mM | 0.6865 mL | 3.4327 mL | 6.8653 mL |
| 10 mM | 0.3433 mL | 1.7163 mL | 3.4327 mL |