1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. BRD9500

BRD9500 

目录号: HY-136350
产品使用指南

BRD9500 是一种有效的,具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂,对 PDE3APDE3BIC50 分别为 10 和 27 nM。具有抗肿瘤活性。

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BRD9500 Chemical Structure

BRD9500 Chemical Structure

CAS No. : 1630760-75-6

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Description

BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1].

IC50 & Target[1]

PDE3A

10 nM (IC50)

PDE3B

27 nM (IC50)

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 EC50 of 1 nM for SK-MEL-3 melanoma cell line viability[1].
BRD9500 exhibits an EC50 of 1.6 nM for HeLa viability[1].
BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells[1].

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].

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.
Molecular Weight

291.32

Formula

C₁₅H₁₈FN₃O₂

CAS No.

1630760-75-6

SMILES

O=C1C[C@@H](C)C(C2=CC=C(N3CCOCC3)C(F)=C2)=NN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BRD9500BRD 9500BRD-9500Phosphodiesterase (PDE)phosphodiesterasesPDE3ASK-MEL-3melanomaPDE3Inhibitorinhibitorinhibit

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产品名称:
BRD9500
目录号:
HY-136350
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