产品
编 号：F762452
分子式：C61H71ClN8O7S
分子量：1095.78
分子式：C61H71ClN8O7S
分子量：1095.78
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规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2316837-08-6
产品详情
生物活性：
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
ARD-61 (25, 50?mg/kg/day; ip; for 75 days) effectively inhibits tumor growthin the MDA-MB-453 xenograft tumor model in male SCID mice. ARD-61 (25?mg/kg; ip; single dose) effectively and rapidly reduces the AR protein in the MDA-MB-453 xenograft tissue, with the effect persisting for at least 24?h. ARD-61 is very effective in reducing the mRNA level of WNT7B in a time-dependent manner. Animal Model:MDA-MB-453 xenograft tumor model in male SCID mice
Dosage:25, 50?mg/kg
Administration:IP; daily; for 75 days
Result:Effectively inhibited tumor growth.
体外研究：
ARD-61 binds to AR protein through its AR antagonist portion and von Hippel-Lindau (VHL)/cullin 2 E3 ligase through its VHL ligand portion to recruit AR protein to cullin 2 for ubiquitination, followed by proteasome-dependent AR degradation.ARD-61 (0.001-100 μM; for 7?days) has IC50 values of 235?nM and 121?nM in the MDA-MB-453 and HCC1428 cell lines, which have the highest AR expression, respectively. ARD-61 demonstrates partial cell growth inhibition, delivering IC50 values of 39, 147, and 380?nM, respectively, in the MCF-7, BT-549 and MDA-MB-415 cell lines, which have a moderate level of AR protein. ARD-61 (25-100000 nM; 6-72 h) induces G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines.ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 and HCC1428 cell lines. ARD-61 (0.01-1000 nM; 6 h) is highly potent and effective in reducing AR protein levels. ARD-61 (0.01-1000 nM; 24 h) reduces the level of PR protein with a DC50 value of 0.15?nM in the T47D cells. ARD-61 has no obvious effect on ER and GR proteins. ARD-61 (1?μM; for 24?h) effectively inhibits Wnt/β-catenin and MYC signaling pathways. ARD-61 (1-1000?nM; for 24?h) not only decreases both phosphorylated HER2 and HER3, but also un-phosphorylated HER2 and HER3 proteins. Efficient knock-down of VHL completely blocks AR degradation induced by ARD-61 (100?nM; 24 h) in both MDA-MB-453 and MCF-7 cell lines.
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
ARD-61 (25, 50?mg/kg/day; ip; for 75 days) effectively inhibits tumor growthin the MDA-MB-453 xenograft tumor model in male SCID mice. ARD-61 (25?mg/kg; ip; single dose) effectively and rapidly reduces the AR protein in the MDA-MB-453 xenograft tissue, with the effect persisting for at least 24?h. ARD-61 is very effective in reducing the mRNA level of WNT7B in a time-dependent manner. Animal Model:MDA-MB-453 xenograft tumor model in male SCID mice
Dosage:25, 50?mg/kg
Administration:IP; daily; for 75 days
Result:Effectively inhibited tumor growth.
体外研究：
ARD-61 binds to AR protein through its AR antagonist portion and von Hippel-Lindau (VHL)/cullin 2 E3 ligase through its VHL ligand portion to recruit AR protein to cullin 2 for ubiquitination, followed by proteasome-dependent AR degradation.ARD-61 (0.001-100 μM; for 7?days) has IC50 values of 235?nM and 121?nM in the MDA-MB-453 and HCC1428 cell lines, which have the highest AR expression, respectively. ARD-61 demonstrates partial cell growth inhibition, delivering IC50 values of 39, 147, and 380?nM, respectively, in the MCF-7, BT-549 and MDA-MB-415 cell lines, which have a moderate level of AR protein. ARD-61 (25-100000 nM; 6-72 h) induces G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines.ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 and HCC1428 cell lines. ARD-61 (0.01-1000 nM; 6 h) is highly potent and effective in reducing AR protein levels. ARD-61 (0.01-1000 nM; 24 h) reduces the level of PR protein with a DC50 value of 0.15?nM in the T47D cells. ARD-61 has no obvious effect on ER and GR proteins. ARD-61 (1?μM; for 24?h) effectively inhibits Wnt/β-catenin and MYC signaling pathways. ARD-61 (1-1000?nM; for 24?h) not only decreases both phosphorylated HER2 and HER3, but also un-phosphorylated HER2 and HER3 proteins. Efficient knock-down of VHL completely blocks AR degradation induced by ARD-61 (100?nM; 24 h) in both MDA-MB-453 and MCF-7 cell lines.
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