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[바이오클론] [MedChemExpress한국독점대리점] BRD9500
바이오클론
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BRD9500
제품 설명 |
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1]. |
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IC50 & Target[1] |
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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. |
분자량
291.32
화학식
C₁₅H₁₈FN₃O₂
CAS No.
1630760-75-6
SMILES
O=C1C[C@@H](C)C(C2=CC=C(N3CCOCC3)C(F)=C2)=NN1
선적
Room temperature in continental US; may vary elsewhere.
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
References
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