ARV-110是一种具有口服生物利用度的特异性雄激素受体（AR）PROTAC降解剂，可导致AR的泛素化和降解。
Cas No.:2222112-77-6
Sample solution is provided at 25 µL, 10mM.
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ARV-110 is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR [1]. ARV-110 can degrade mutant AR proteins and inhibit the expression of AR target genes PSA and FKBP5[2]. ARV-110 has been widely used in prostate cancer models to inhibit tumor growth and reduce the expression of the oncogenic protein Erg[3].
In vitro, ARV-110 treatment for 4 days significantly inhibited the viability of 22Rv1 cells, LNCaP cells and VCap cells, with IC50 values of 0.316μM, 0.124μM and 0.125μM, respectively[4]. Treatment with 100nM ARV-110 for 48 hours significantly induced AR degradation in LNCaP cells and inhibited the synthesis of PSA protein[5].
In vivo, oral administration of 0.5mg/kg dose of ARV-110 daily for 14 days significantly inhibited tumor growth in a DU145 cell-xenograft mouse model[6]. For 8 consecutive weeks, subcutaneous administration of 1mg/kg dose of ARV-110 daily reduced the levels of AR proteins in white adipose tissue (WAT), kidneys, liver and ovaries of the mouse model of polycystic ovary syndrome, mitigated the increase in body weight, fat mass, kidney mass, WAT mass and circulating leptin levels induced by dihydrotestosterone (DHT), and altered glucose homeostasis[7]. Subcutaneous injection of 1mg/kg/day dose of ARV-110 for 8 weeks can alleviate DHT-induced obesity, glucose intolerance, as well as kidney hypertrophy and damage in mice[8].
References:
[1] Nguyen T T L, Kim J W, Choi H I, et al. Development of an LC-MS/MS Method for ARV-110, a PROTAC Molecule, and Applications to Pharmacokinetic Studies[J]. Molecules, 2022, 27(6): 1977.
[2] Zhang Y, Ming A, Wang J, et al. PROTACs targeting androgen receptor signaling: Potential therapeutic agents for castration-resistant prostate cancer[J]. Pharmacological Research, 2024, 205: 107234.
[3] Neklesa T, Snyder L B, Willard R R, et al. ARV-110: An androgen receptor PROTAC degrader for prostate cancer[J]. Cancer research, 2018, 78(13_Supplement): 5236-5236.
[4] Chen Z, Wang M, Wu D, et al. Discovery of CBPD-268 as an exceptionally potent and orally efficacious CBP/p300 PROTAC degrader capable of achieving tumor regression[J]. Journal of Medicinal Chemistry, 2024, 67(7): 5275-5304.
[5] Snyder L B, Neklesa T K, Willard R R, et al. Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting Chimera Androgen Receptor Degrader[J]. Molecular cancer therapeutics, 2025, 24(4): 511-522.
[6] He Y, Zheng Y, Zhu C, et al. Radioactive ADME demonstrates ARV-110’s high druggability despite low oral bioavailability[J]. Journal of Medicinal Chemistry, 2024, 67(16): 14277-14291.
[7] Basnet J, Rezq S, Huffman A M, et al. Androgen receptor PROTAC ARV-110 ameliorates metabolic complications in a mouse model of polycystic ovary syndrome[J]. Endocrinology, 2025, 166(7): bqaf091.
[8] Basnet J, Rezq S, Huffman A M, et al. MON-179 Renal and Hepatic Effects of Androgen Receptor Downregulation by PROTAC ARV-110 in a Mouse Model of Polycystic Ovary Syndrome[J]. Journal of the Endocrine Society, 2025, 9(Supplement_1): bvaf149. 1911.
ARV-110是一种具有口服生物利用度的特异性雄激素受体（AR）PROTAC降解剂，可导致AR的泛素化和降解[1]。ARV-110能够降解突变型AR蛋白，并抑制AR靶基因PSA和FKBP5的表达[2]。ARV-110已被广泛用于前列腺癌模型，以抑制肿瘤生长并降低致癌蛋白Erg的表达[3]。
在体外，ARV-110处理4天显著抑制了22Rv1细胞、LNCaP细胞和VCap细胞的活力，IC50值分别为0.316µM、0.124µM和0.125µM[4]。使用100nM的ARV-110处理48小时，显著诱导了LNCaP细胞中AR的降解，并抑制了PSA蛋白的合成[5]。
在体内，每日口服0.5mg/kg剂量的ARV-110，持续14天，显著抑制了DU145细胞异种移植小鼠模型中的肿瘤生长[6]。连续8周每日皮下注射1mg/kg剂量的ARV-110，降低了多囊卵巢综合征小鼠模型中白色脂肪组织（WAT）、肾脏、肝脏和卵巢的AR蛋白水平，减轻了二氢睾酮（DHT）诱导的体重、脂肪量、肾脏质量、WAT质量和循环瘦素水平的增加，并改变了葡萄糖稳态[7]。给小鼠每日皮下注射1mg/kg剂量的ARV-110，持续8周，可缓解DHT诱导的肥胖、葡萄糖耐受不良，以及肾脏肥大和损伤[8]。
| Cell experiment [1]: | |
Cell lines | LNCaP cell |
Preparation Method | LNCaP cells were cultured in RPMI-1640 medium supplemented with 5% charcoal-stripped fetal bovine serum (FBS) and penicillin-streptomycin (1%) at 37°C in a humidified atmosphere containing 5% CO2. The cells were cultured in 96-well plates overnight and incubated with different concentrations of ARV-110 (0.1, 0.3, 1, 3, 10, 30, 100 and 300nM) for 24 hours and analyzed the level of AR. |
Reaction Conditions | 0.1, 0.3, 1, 3, 10, 30, 100 and 300nM; 24h |
Applications | ARV-110 treatment degraded the wild-type AR in the LNCaP cells in a dose-dependent manner |
| Animal experiment [2]: | |
Animal models | Male BALB/c nude mice |
Preparation Method | Thirty 4-week-old male BALB/c nude mice were raised under SPF conditions. The environmental temperature was maintained at 22-26°C, the relative humidity was 50%-60%, and the light/dark cycle was 12 hours. 1×107 DU145 cells were subcutaneously injected into the proximal part of the right axilla of the nude mice at a volume of 100μl. After 4 weeks of tumor growth, the mice were divided into 3 groups: the vehicle group, the positive control group (enzalutamide; 20mg/kg/day; p.o.), and the ARV-110 treatment group (0.5mg/kg/day; p.o.). The entire treatment process lasted for 14 days, and the tumor size was measured every day. |
Dosage form | 0.5mg/kg/day for 14 days; p.o. |
Applications | ARV-110 treatment significantly inhibited tumor growth in the DU145 cell-xenograft mouse model. |
References: | |
| Cas No. | 2222112-77-6 | SDF | |
| 别名 | ARV-110 | ||
| 分子式 | C41H43ClFN9O6 | 分子量 | 812.29 |
| 溶解度 | DMSO : 26.67 mg/mL (32.83 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C) | 储存条件 | Store at-20°C, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2311 mL | 6.1554 mL | 12.3109 mL |
| 5 mM | 246.2 μL | 1.2311 mL | 2.4622 mL |
| 10 mM | 123.1 μL | 615.5 μL | 1.2311 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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