MST-312是一种强效的端粒酶抑制剂，IC50值为0.67µM。
Cas No.:368449-04-1
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
MST-312 is a potent telomerase inhibitor, with an IC50 value of 0.67μM [1]. MST-312 reduces the activity of telomerase in cells, causing telomere dysfunction, leading to DNA damage and cell growth arrest[2]. MST-312 has been widely used to inhibit the proliferation of leukemia cells, and new combined therapies have been developed to suppress the vitality of tumor cells[3].
In vitro, MST-312 treatment for 72 hours significantly inhibited the viability of PA-1 cells, A2780 cells and OVCAR3 cells, with IC50 values of 4.2μM, 3.9μM and 7.1μM, respectively[4]. Treatment with 8μM MST-312 for 48 hours reduced the cell viability and metabolic activity of U-266 cells and induced cell apoptosis[5]. Treatment with 4μM MST-312 for 48 hours inhibited the proliferation of Jurkat cells and downregulated the expressions of CCND1, MDM2, MYC and HSP90AA1[6]. Treatment with 100μM MST-312 for 18 hours inhibited the replication of HSV-1 virus in HEp-2 cells, reduced the number of cells exhibiting cytopathic effects, and decreased the accumulation of early and late viral proteins[7].
In vivo, MST-312 treatment via oral administration (400mg/kg; 5 times a week) for 6 weeks inhibited the growth of tumor volume in the HBC-4 cell-xenograft mouse model and caused weight loss in mice[8].
References:
[1] Seimiya H, Oh-hara T, Suzuki T, et al. Telomere shortening and growth inhibition of human cancer cells by novel synthetic telomerase inhibitors MST-312, MST-295, and MST-199[J]. Molecular cancer therapeutics, 2002, 1(9): 657-665.
[2] Gurung R L, Lim S N, Low G K M, et al. MST-312 alters telomere dynamics, gene expression profiles and growth in human breast cancer cells[J]. Journal of Nutrigenetics and Nutrigenomics, 2015, 7(4-6): 283-298.
[3] Ghasemimehr N, Farsinejad A, Khalilabadi R M, et al. The telomerase inhibitor MST-312 synergistically enhances the apoptotic effect of doxorubicin in pre-B acute lymphoblastic leukemia cells[J]. Biomedicine & Pharmacotherapy, 2018, 106: 1742-1750.
[4] Fernandes S G, Gala K, Khattar E. Telomerase inhibitor MST-312 and quercetin synergistically inhibit cancer cell proliferation by promoting DNA damage[J]. Translational Oncology, 2023, 27: 101569.
[5] Ameri Z, Ghiasi S, Farsinejad A, et al. Telomerase inhibitor MST-312 induces apoptosis of multiple myeloma cells and down-regulation of anti-apoptotic, proliferative and inflammatory genes[J]. Life Sciences, 2019, 228: 66-71.
[6] Bahmei A, Karimi F, Mahini S M, et al. Targeting telomerase with MST-312 leads to downregulation of CCND1, MDM2, MYC, and HSP90AA1 and induce apoptosis in Jurkat cell line[J]. Medical Oncology, 2024, 41(11): 267.
[7] Haberichter J, Roberts S, Abbasi I, et al. The telomerase inhibitor MST-312 interferes with multiple steps in the herpes simplex virus life cycle[J]. Journal of Virology, 2015, 89(19): 9804-9816.
[8] Fujiwara C, Muramatsu Y, Nishii M, et al. Cell-based chemical fingerprinting identifies telomeres and lamin A as modifiers of DNA damage response in cancer cells[J]. Scientific reports, 2018, 8(1): 14827.
MST-312是一种强效的端粒酶抑制剂，IC50值为0.67µM[1]。MST-312降低细胞中端粒酶的活性，导致端粒功能障碍，从而引起DNA损伤和细胞生长停滞[2]。MST-312已被广泛用于抑制白血病细胞增殖，并用以开发新的联合疗法来抑制肿瘤细胞的活力[3]。
在体外，MST-312处理72小时显著抑制了PA-1细胞、A2780细胞和OVCAR3细胞的活力，IC50值分别为4.2µM、3.9µM和7.1µM[4]。使用8µM的MST-312处理48小时，降低了U-266细胞的活力和代谢活性，并诱导了细胞凋亡[5]。使用4µM的MST-312处理48小时，抑制了Jurkat细胞的增殖，并下调了CCND1、MDM2、MYC和HSP90AA1的表达[6]。使用100µM的MST-312处理18小时，抑制了HSV-1病毒在HEp-2细胞中的复制，减少了表现出细胞病变效应的细胞数量，并降低了早期和晚期病毒蛋白的积累[7]。
在体内，每周5次口服给予MST-312（400mg/kg），持续6周，抑制了HBC-4细胞异种移植小鼠模型中的肿瘤体积生长，并导致小鼠体重下降[8]。
| Cell experiment [1]: | |
Cell lines | A2780 cells |
Preparation Method | A2780 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). A2780 cells (8×104 cells) were plated using 96-well plates and subjected to incubation for 24h in a 5% CO2 incubator. Incubation was followed by treatment with different doses of MST-312 (0.1, 1, 10, and 100μM) for 72h and cell viability was measured. |
Reaction Conditions | 0.1, 1, 10, and 100μM; 72h |
Applications | MST-312 treatment decreased the cell viability of A2780 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/cAJcl-nu nude mice |
Preparation Method | The HBC-4 cells were subcutaneously implanted into the right abdomen of 9-week-old BALB/cAJcl-nu nude mice. The experiment began when the tumor volume reached 50-150mm3 (on day 0). In the experimental group mice, MST-312 was administered at a dose of 400mg/kg, 5 times a week, once a day, for 6 weeks. The control group mice (n=6) received the same volume of normal saline as the experimental group mice (n=6). The tumor growth was monitored. The length (L) and width (W) of the tumor were measured, and the tumor volume (TV) was calculated using the formula TV=LW2/2. |
Dosage form | 400mg/kg; 5 times a week for 6 weeks; p.o. |
Applications | MST-312 treatment inhibited the growth of tumor volume in a HBC-4 cell-xenograft mouse model and caused weight loss in mice. |
References: | |
| Cas No. | 368449-04-1 | SDF | |
| 别名 | Telomerase Inhibitor IX | ||
| 化学名 | N,N'-1,3-phenylenebis[2,3-dihydroxy-benzamide | ||
| Canonical SMILES | OC1=C(O)C(C(NC2=CC=CC(NC(C3=C(O)C(O)=CC=C3)=O)=C2)=O)=CC=C1 | ||
| 分子式 | C20H16N2O6 | 分子量 | 380.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:40): 0.025 mg/ml,Ethanol: 0.2 mg/ml | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6288 mL | 13.1441 mL | 26.2881 mL |
| 5 mM | 525.8 μL | 2.6288 mL | 5.2576 mL |
| 10 mM | 262.9 μL | 1.3144 mL | 2.6288 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet