STAT3-IN-1是一种强效、选择性且口服有效的STAT3抑制剂，在HT29和MDA-MB-231细胞中的IC50值分别为1.82µM和2.14µM。
Cas No.:2059952-75-7
Sample solution is provided at 25 µL, 10mM.
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STAT3-IN-1 is a potent, selective, and orally active inhibitor of STAT3 with IC50 values of 1.82μM and 2.14μM in HT29 and MDA-MB-231 cells, respectively [1]. STAT3-IN-1 inhibits both STAT3 acetylation and phosphorylation, leading to increased NKG2D ligand expression and decreased IL-10 levels[1-2]. STAT3-IN-1 has been widely used to induce growth arrest and tumor cell death in Meta4 organoids[3].
In vitro, STAT3-IN-1 treatment at 1μM for 8h significantly inhibited the decrease in Nos2 mRNA levels and the increase in IL-1β and IL-6 levels caused by 100μg/ml zymosan in mouse primary bone marrow dendritic cells (BMDCs)[4]. STAT3-IN-1 treatment (3μM) for 48h suppressed the cell migration of DU145 cells induced by CCL5 and retarded the upregulation of Snail and TWIST[5].
In vivo, STAT3-IN-1 treatment via oral administration at a dose of 20mg/kg daily for 14 days significantly inhibited tumor growth in a xenograft model of 4T1 cells without affecting body weight[6]. Injecting STAT3-IN-1 (5mg/kg) and temozolomide (5mg/kg) intratumorally every 5 days for 10 consecutive days can significantly inhibit the tumor growth of A375 cell-xenograft mice with overexpressed RPL18 and improve the survival rate[7].
References:
[1] Hu Y, Dong Z, Liu K. Unraveling the complexity of STAT3 in cancer: molecular understanding and drug discovery[J]. Journal of Experimental & Clinical Cancer Research, 2024, 43(1): 23.
[2] Jia Z, Xiao B, Li J, et al. BTK inhibitors enhance NKG2D ligand expression by regulating IL-10/STAT3 pathway in activated non-GCB diffuse large B-cell lymphoma cells[J]. Anti-Cancer Drugs, 2025, 36(5): 374-382.
[3] Kim H, Jang B, Zhang C, et al. Targeting stem cells and dysplastic features with dual MEK/ERK and STAT3 suppression in gastric carcinogenesis[J]. Gastroenterology, 2024, 166(1): 117-131.
[4] Wu H, Yin X, Zhao X, et al. HDAC11 negatively regulates antifungal immunity by inhibiting Nos2 expression via binding with transcriptional repressor STAT3[J]. Redox Biology, 2022, 56: 102461.
[5] Ma J, Shayiti F, Ma J, et al. Tumor‐associated macrophage‐derived CCL5 promotes chemotherapy resistance and metastasis in prostatic cancer[J]. Cell biology international, 2021, 45(10): 2054-2062.
[6] Li S, Zhang W, Yang Y, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein[J]. European journal of medicinal chemistry, 2016, 124: 1006-1018.
[7] Zuo C, Hu C, Jiang X, et al. RPL18 promotes melanoma progression and drug resistance via BTF3/STAT3-dependent mechanisms and immune modulation[J]. iScience, 2026, 29(1).
STAT3-IN-1是一种强效、选择性且口服有效的STAT3抑制剂，在HT29和MDA-MB-231细胞中的IC50值分别为1.82µM和2.14µM [1]。STAT3-IN-1可同时抑制STAT3的乙酰化和磷酸化，导致NKG2D配体表达增加以及IL-10水平降低[1-2]。STAT3-IN-1已被广泛用于在Meta4类器官中诱导生长停滞和肿瘤细胞死亡[3]。
在体外，使用1µM的STAT3-IN-1处理小鼠原代骨髓树突状细胞（BMDCs）8小时，显著抑制了100µg/ml酵母聚糖引起的Nos2 mRNA水平下降以及IL-1β和IL-6水平升高[4]。STAT3-IN-1处理（3µM）48小时，抑制了CCL5诱导的DU145细胞迁移，并延缓了Snail和TWIST的上调[6]。
在体内，每日口服给予20mg/kg剂量的STAT3-IN-1，持续14天，显著抑制了4T1细胞异种移植模型中的肿瘤生长，且未影响体重[6]。每5天瘤内注射一次STAT3-IN-1（5mg/kg）和temozolomide（5mg/kg），连续10天，可显著抑制过表达RPL18的A375细胞异种移植小鼠的肿瘤生长，并提高存活率[7]。
| Cell experiment [1]: | |
Cell lines | DU145 cells |
Preparation Method | DU145 cells were cultured in RPMI 1640 medium containing 10% fetal bovine serum (FBS) at 37℃ in the presence of 5% CO2. Cells migrating assay was detected using 8-μm trans-well chambers. DU145 cells were pretreated with STAT3-IN-1 (3μM) and CCL5 (100ng/ml) for 48h. 5×104 cells in 150μl non-serum culture medium were seeded into the upper chambers. A total of 800μl culture medium containing 10% FBS medium was added into the lower chambers. Twenty-four hours later, trans-wells were washed with phosphate-buffered saline (PBS), fixed with formalin, and stained with 0.1% crystal violet. Cells were counted in three random fields per well under a ×100 microscope. |
Reaction Conditions | 3μM; 48h |
Applications | STAT3-IN-1 treatment suppressed the cell migration of DU145 cells induced by CCL5. |
| Animal experiment [2]: | |
Animal models | Female Kunming mice |
Preparation Method | Adult female Kunming mice (4-6 weeks of age) were group-housed in polysulfone cages with bedding material, and were housed in a room with controlled humidity (50±10%) and temperature (25±3°C) under a 12/12h light/dark cycle. All mice were adaptively fed for one week. Freshly harvested breast cancer cells 4T1 (2.5×106 cells per mouse, resuspended in 100μl PBS) were injected into the armpit of the mice. The mice were given 20mg/kg STAT3-IN-1, or vehicle p.o. once daily. Body weights were measured every other day. On the 14th day, all mice were killed, and the tumor was segregated and weighed. |
Dosage form | 20mg/kg/day for 14 days; p.o. |
Applications | STAT3-IN-1 treatment inhibited tumor growth in a xenograft model of 4T1 cells without affecting body weight. |
References: | |
| Cas No. | 2059952-75-7 | SDF | |
| Canonical SMILES | COC1=CC(OC)=CC(/C=C/C2=CC=C(NC(/C=C/C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=C1 | ||
| 分子式 | C28H29NO6 | 分子量 | 475.53 |
| 溶解度 | DMSO: 125 mg/mL (262.86 mM) | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1029 mL | 10.5146 mL | 21.0292 mL |
| 5 mM | 420.6 μL | 2.1029 mL | 4.2058 mL |
| 10 mM | 210.3 μL | 1.0515 mL | 2.1029 mL |
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| 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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