BRD9500|cas:1630760-75-6|西域试剂

BRD9500,99.60%

产品编号：Bellancom-136350| CAS NO：1630760-75-6| 分子式：C₁₅H₁₈FN₃O₂| 分子量：291.32

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货号	价格	库存与货期
Bellancom-136350	￥2900.00	杭州北京（现货）
Bellancom-136350	￥4800.00	杭州北京（现货）
Bellancom-136350	￥13500.00	杭州北京（现货）
Bellancom-136350	￥20600.00	杭州北京（现货）

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BRD9500

产品介绍

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 PDE3A 和 PDE3B 的 IC₅₀ 分别为 10 和 27 nM。具有抗肿瘤活性。

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.

体外研究

BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12.
BRD9500 exhibits an EC₅₀ of 1 nM for SK-MEL-3 melanoma cell line viability.
BRD9500 exhibits an EC₅₀ of 1.6 nM for HeLa viability.
BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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.
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.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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。