BRD9500

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BRD9500  纯度: 99.60%

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。

BRD9500

BRD9500 Chemical Structure

CAS No. : 1630760-75-6

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5 mg ¥2900 In-stock
10 mg ¥4800 In-stock
50 mg ¥13500 In-stock
100 mg ¥20600 In-stock
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500 mg   询价  

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BRD9500 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Targeted Diversity Library

生物活性

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)

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

291.32

Formula

C15H18FN3O2

CAS 号

1630760-75-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (171.63 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.58 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Timothy A Lewis, et al. Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing. ACS Med Chem Lett. 2019 Oct 18;10(11):1537-1542.

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