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BRD9500

Catalog No. T60603 CAS 1630760-75-6

BRD9500 is an orally active inhibitor of phosphodiesterases 3 (PDE3) with IC 50 s of 10 and 27 nM for PDE3A and PDE3B, respectively. BRD9500 is active in an SK-MEL-3 xenograft model of cancer [1].

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BRD9500, CAS 1630760-75-6

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 274.00
25 mg	6-8 weeks	$ 854.00
50 mg	6-8 weeks	$ 1,110.00
100 mg	6-8 weeks	$ 1,700.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 263.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BRD9500 is an orally active inhibitor of phosphodiesterases 3 (PDE3) with IC 50 s of 10 and 27 nM for PDE3A and PDE3B, respectively. BRD9500 is active in an SK-MEL-3 xenograft model of cancer [1].
In vitro	As an analog of DNMDP, BRD9500 effectively and selectively targets PDE3A and PDE3B, disrupting cancer cell viability by facilitating the interaction between PDE3A/B and SLFN12. This compound has demonstrated potent activity against the SK-MEL-3 melanoma cell line, with an EC50 of 1 nM, and against HeLa cells, with an EC50 of 1.6 nM. Furthermore, at a concentration of 10 μM over 8 hours, BRD9500 stabilizes the PDE3A-SLFN12 interaction in HeLa cells, evidenced by a Western Blot Analysis. This analysis revealed clear detection of the SLFN12-V5 fusion protein via coimmunoprecipitation and immunoblotting with an anti-V5 antibody, confirming the compound's targeted mechanism of action.
In vivo	BRD9500, administered orally at dosages of 10, 20, and 50 mg/kg, effectively inhibits the growth of SK-MEL-3 melanoma in mouse models, demonstrating potent antitumor activity, particularly at 50 mg/kg. Notably, it exhibits high plasma concentrations when given either intravenously (iv) at 1 mg/kg or orally (po) at 2 mg/kg, persisting for over eight hours. This pharmacokinetic profile, combined with its tolerability—evidenced by the absence of significant weight loss or toxicities in treated animals—positions BRD9500 as a promising agent for in vivo xenograft experimentation. The study utilized female NMRI nude mice implanted with SK-MEL-3 melanoma cell tumor xenografts, applying oral doses of 10 and 20 mg/kg twice daily and 50 mg/kg once daily, with the highest dose yielding the most pronounced antitumor effects.

Molecular Weight	291.32
Formula	C15H18FN3O2
CAS No.	1630760-75-6

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BRD9500 1630760-75-6 inhibitor inhibit

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