ARD-2128|2222111-87-5|-陌孚医药/Medlife

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ARD-2128

目录号: PL03287 纯度: ≥99%

CAS No. :2222111-87-5

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中文名称	ARD-2128
英文名称	ARD-2128
英文别名	N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-;ARD-2128
Cas No.	2222111-87-5
分子式	C₄₅H₅₀ClN₇O₆
分子量	820.37
包装储存	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情	ARD-2128 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂。ARD-2128 可有效降低 AR 蛋白并抑制肿瘤组织中 AR 调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。ARD-2128 作用在前列腺癌的研究上。
生物活性	ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
性状	Solid
IC50 & Target[1][2]	IC50: 4 nM (VCaP), 5 μM (LNCaP)
体外研究(In Vitro)	ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values of 4 nM and 5 nM, respectively. ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours. ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice. ARD-2128 (5mg/kg; p.o.) treatment shows the C max , AUC 0-t and t 1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献	[1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmed

溶解度数据	In Vitro: DMSO : 100 mg/mL (121.90 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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