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产品介绍
产品信息
商品描述
Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.
分子量
427.27
纯度
98%
可溶性
DMSO : 130 mg/mL (304.26 mM; Need ultrasonic)
In vitro(体外研究)
Y06036 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC50: 0.29-2.6 μΜ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06036 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels.Cell Viability AssayCell Line:LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells Concentration:0.001-100 μMIncubation Time:96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaPResult:Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 1.06, 2.62, 1.50, 0.63 μM, respectively.
In vivo(体内研究)
Y06036 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC50: 0.29-2.6 μΜ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06036 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels.Cell Viability AssayCell Line:LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells Concentration:0.001-100 μMIncubation Time:96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaPResult:Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 1.06, 2.62, 1.50, 0.63 μM, respectively.
背景
分子式
C16H15BrN2O5S
CAS号
1832671-96-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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