Tasquinimod是一种具有口服活性的组蛋白去乙酰化酶4（HDAC4）和S100 钙结合蛋白A9（S100A9）抑制剂。
Cas No.:254964-60-8
Sample solution is provided at 25 µL, 10mM.
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Tasquinimod is an orally active inhibitor of histone deacetylase 4 (HDAC4) and S100 calcium-binding protein A9 (S100A9)[1]. Tasquinimod inhibits angiogenesis and reduces immunosuppression within tumors, and is commonly used in the research and treatment of metastatic castration-resistant prostate cancer (mCRPC)[2,3,4].
In vitro, treatment of SKOV3/DDP cells with Tasquinimod (40μM) for 12-48h resulted in significantly downregulated Bcl-2 expression and significantly upregulated cleaved-Caspase-3 expression compared to controls. Overexpression of HDAC4 partially reversed the pro-apoptotic effect of Tasquinimod[5]. Treatment of SKOV3 cells with Tasquinimod (40μM) for 48h reduced the relative scratch width and inhibited cell migration ability[6].
In vivo, oral administration of Tasquinimod (10mg/kg/day) for 9 weeks in mice with intratibial injections of LNCaP-19 cells reduced the tumor incidence in bone from 7/10 in the control group to 2/10 in the treatment group[7]. Oral administration of Tasquinimod (10mg/kg/day) for 3 weeks in LNCaP tumor-bearing mice significantly increased TSP1 protein levels in tumor tissues, and the ratio of intact TSP1 (approximately 150-160kDa) to β-actin was markedly increased in the treatment group[8].
References:
[1] Fan R, Satilmis H, Vandewalle N, et al. Tasquinimod suppresses tumor cell growth and bone resorption by targeting immunosuppressive myeloid cells and inhibiting c-MYC expression in multiple myeloma[J]. Journal for Immunotherapy of Cancer, 2023, 11(1): e005319.
[2] Raymond E, Dalgleish A, Damber J E, et al. Mechanisms of action of tasquinimod on the tumour microenvironment[J]. Cancer Chemotherapy and Pharmacology, 2014, 73(1): 1-8.
[3] Gupta N, Al Ustwani O, Shen L, et al. Mechanism of action and clinical activity of tasquinimod in castrate-resistant prostate cancer[J]. OncoTargets and Therapy, 2014: 223-234.
[4] Mehta A R, Armstrong A J. Tasquinimod in the treatment of castrate-resistant prostate cancer–current status and future prospects[J]. Therapeutic Advances in Urology, 2016, 8(1): 9-18.
[5] Li Z, Wu Y H, Guo Y Q, et al. Tasquinimod promotes the sensitivity of ovarian cancer cells to cisplatin by down-regulating the HDAC4/p21 pathway[J]. The Korean Journal of Physiology & Pharmacology, 2025, 29(2): 191-204.
[6] Lin Y, Liu Y Q, Zhu K A, et al. Tasquinimod enhances the sensitivity of ovarian cancer cells to cisplatin by regulating the Nur77-Bcl-2 apoptotic pathway[J]. Advances in Clinical and Experimental Medicine, 2024, 33(2): 151-161.
[7] Jennbacken K, Welén K, Olsson A, et al. Inhibition of metastasis in a castration resistant prostate cancer model by the quinoline-3-carboxamide tasquinimod (ABR-215050)[J]. The Prostate, 2012, 72(8): 913-924.
[8] Olsson A, Björk A, Vallon-Christersson J, et al. Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors[J]. Molecular Cancer, 2010, 9(1): 107.
Tasquinimod是一种具有口服活性的组蛋白去乙酰化酶4（HDAC4）和S100 钙结合蛋白A9（S100A9）抑制剂[1]。Tasquinimod可抑制血管生成，并减少肿瘤内的免疫抑制作用，通常用于转移性去势抵抗性前列腺癌（mCRPC）的研究和治疗[2,3,4]。
在体外，Tasquinimod（40μM）处理SKOV3/DDP细胞12-48h，较对照Bcl-2表达显著下调，cleaved-Caspase-3表达显著上调，过表达HDAC4可部分逆转Tasquinimod的促凋亡效应[5]。Tasquinimod（40μM）处理SKOV3细胞48h，相对划痕宽度减小，细胞迁移能力被抑制[6]。
在体内，Tasquinimod（10mg/kg/day）通过口服治疗胫骨内注射LNCaP-19细胞的小鼠9周，肿瘤在骨内的出现率从对照组的7/10只降至治疗组的2/10只[7]。Tasquinimod（10mg/kg/day）通过口服治疗LNCaP荷瘤小鼠3周，肿瘤组织中的TSP1蛋白水平显著升高，完整TSP1（约150-160kD）与β-actin的比值在治疗组中明显增加[8]。
| Cell experiment [1]: | |
Cell lines | SKOV3 cells |
Preparation Method | SKOV3 cells were treated with 40μM Tasquinimod for 48h, then cell migration was assessed using the scratch-wound assay. Linear wounds were scratched using a sterile pipette tip, and the relative scratch width was measured after 48h of incubation. |
Reaction Conditions | 40μM; 48h |
Applications | Treatment with Tasquinimod reduced the relative scratch width and inhibited cell migration. |
| Animal experiment [2]: | |
Animal models | Nude BALB/c mice bearing subcutaneous LNCaP prostate tumor cells |
Preparation Method | Nude mice were subcutaneously inoculated with LNCaP cells. Tasquinimod (10mg/kg/day) was administered orally via drinking water for 3 weeks. Animals were euthanized on day 28 after inoculation, and tumor tissues were excised. TSP1 protein levels were assessed by western blot, with β-actin as internal control. |
Dosage form | 10mg/kg/day; 3 weeks; p.o. |
Applications | Treatment with Tasquinimod significantly increased the level of TSP1 protein in tumor tissues, and the ratio of intact TSP1 (approximately 150-160kDa) to β-actin was significantly increased. |
References: | |
| Cas No. | 254964-60-8 | SDF | |
| 别名 | 他喹莫德; ABR-215050 | ||
| 化学名 | 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]quinoline-3-carboxamide | ||
| Canonical SMILES | CN1C2=C(C(=CC=C2)OC)C(=C(C1=O)C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)O | ||
| 分子式 | C20H17F3N2O4 | 分子量 | 406.36 |
| 溶解度 | ≥ 20.318 mg/mL in DMSO, ≥ 4.75 mg/mL in EtOH with ultrasonic and warming | 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 | 2.4609 mL | 12.3044 mL | 24.6087 mL |
| 5 mM | 492.2 μL | 2.4609 mL | 4.9217 mL |
| 10 mM | 246.1 μL | 1.2304 mL | 2.4609 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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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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