ALV2是一种有效和选择性的Helios降解剂，ALV2可以结合CRBN（IC50=0.57μM）。
Cas No.:2438124-95-7
Sample solution is provided at 25 µL, 10mM.
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ALV2 is an effective and selective degrader of Helios (IKZF2). ALV2 binds to CRBN with an IC50 of 0.57μM[1-2]. Helios is a zinc-finger transcription factor that maintains a stable regulatory T cell (Treg) phenotype within the inflammatory tumor microenvironment. ALV2 is used in research investigating the regulation of T cell function and the tumor immune microenvironment[3-4].
In vitro, ALV2 (1μM) was used to pre-treat human naive CD4+ T cells for 5 days, followed by activation with anti-CD3/CD28 antibodies for 2 days. This treatment significantly upregulated the production of CD25 and effector cytokines (such as IL-21 and IFNγ), and enhanced the ability of these cells to infiltrate inflammatory tissues in a human-synovial tissue-mouse chimeric model[5]. In RAW 264.7 murine macrophages infected with Salmonella for 1 hour, ALV2 (10μM; 24-hour treatment) significantly reduced the secretion of tumor necrosis factor-alpha (TNF-α)[6].
In vivo, in a mouse model with the humanized CrbnI391Vgenotype, administration of ALV2 via intraperitoneal injection (100mg/kg; twice daily; for 7 days) significantly reduced the protein levels of Helios (IKZF2) in splenic CD4+ FoxP3+ regulatory T cells (Tregs), without affecting Ikaros (IKZF1) levels[7].
References:
[1] Zhang Y, Li L, Xu J, et al. A Novel Paradigm for Targeting Challenging Targets: Advancing Technologies and Future Directions of Molecular Glue Degraders. Molecules (Basel, Switzerland). 2026 Jan;31(3):459.
[2] Słabicki M, Park J, Nowak RP, et al. Expanding the druggable zinc-finger proteome defines properties of drug-induced degradation. Molecular Cell. 2025 Aug;85(16):3184-3201.e14.
[3] Xue F, Zhang M, Li S, et al. SE(3)-equivariant ternary complex prediction towards target protein degradation. Nature Communications. 2025 Jul;16(1):5514.
[4] Chen Z, Dhruv H, Zhang X, et al. Development of PVTX-405 as a potent and highly selective molecular glue degrader of IKZF2 for cancer immunotherapy. Nature Communications. 2025 May;16(1):4095.
[5] Zhang H, Jadhav RR, Cao W, et al. Aging-associated HELIOS deficiency in naive CD4+ T cells alters chromatin remodeling and promotes effector cell responses. Nat Immunol. 2023 Jan;24(1):96-109.
[6] Santelices J, Schultz A, Walker A, et al. Targeting deubiquitinating enzymes and ubiquitin pathway modulators to enhance host defense against bacterial infections. mBio. 2025 Oct 8;16(10):e0031225.
[7] Wang ES, Verano AL, Nowak RP, et al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.
ALV2是一种有效和选择性的Helios降解剂，ALV2可以结合CRBN（IC50=0.57μM）[1-2]。Helios是一种锌指转录因子，可以在炎症性肿瘤微环境中维持稳定的Treg细胞表型。ALV2可用于调节T细胞功能和肿瘤免疫微环境的相关研究[3-4]。
在体外，ALV2（1μM）体外预处理人源初始CD4+ T细胞5天，随后用抗CD3/CD28抗体激活2天，显著上调CD25和效应细胞因子（如IL-21和IFNγ）的产生，并增强这些细胞在人类-滑膜组织-小鼠嵌合模型中向炎症组织的浸润能力[5]。以沙门氏菌（Salmonella）感染鼠RAW 264.7巨噬细胞1小时后，ALV2（10μM；处理细胞24小时）显著降低肿瘤坏死因子α（TNF-α）的分泌[6]。
在体内，对人源化CRBN（humanized CrbnI391V）基因型的小鼠模型，通过腹腔注射给药ALV2（100mg/kg；每日两次；共7天），显著降低脾脏组织中CD4+ FoxP3+ 调节性T细胞的Helios（IKZF2）的蛋白水平，同时不影响Ikaros（IKZF1）的水平[7]。
| Cell experiment [1]: | |
Cell lines | RAW 264.7 macrophages (a murine macrophage cell line) |
Preparation Method | RAW 264.7 macrophages were cultured in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin. For high-throughput screening, cells were seeded into 96-well plates and infected with green fluorescent protein (GFP)-labeled SalmonellaTyphimurium UK-1. Following infection, cells were treated with ALV2 (10μM). |
Reaction Conditions | 10μM; 2 or 24 hours. |
Applications | ALV2 significantly reduced the secretion of TNF-α. |
| Animal experiment [2]: | |
Animal models | Humanized CrbnI391Vmice (a mouse model with a CRBN mutation that renders it permissive to IMiD-induced degradation). |
Preparation Method | Mice were treated with ALV2 (100mg/kg; twice daily for 7 days) via intraperitoneal injection. |
Dosage form | 100mg/kg; i.p.; twice daily for 7 days. |
Applications | ALV2 administration induced selective and significant degradation of the Helios (IKZF2) protein in splenic CD4+ FoxP3+ regulatory T cells (Tregs). |
References: | |
| Cas No. | 2438124-95-7 | SDF | |
| 分子式 | C26H26ClN5O5 | 分子量 | 523.97 |
| 溶解度 | DMSO : 160 mg/mL (305.36 mM; Need ultrasonic)|Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| 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 | 1.9085 mL | 9.5425 mL | 19.0851 mL |
| 5 mM | 381.7 μL | 1.9085 mL | 3.817 mL |
| 10 mM | 190.9 μL | 954.3 μL | 1.9085 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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