OM-153
目录号 : GC67906OM-153 是一种有效的，具有口服活性的 tankyrase 抑制剂，对 tankyrase 1 和 tankyrase 2 (TNKS1/2) 的 IC50 分别为 13 nM 和 2 nM。OM-153 抑制基于荧光素酶的 Wnt/β-catenin 信号转导报告基因活性，IC50 值为 0.63 nM。OM-153 抑制 COLO 320DM 中的 Wnt/β-catenin 信号转导和增殖。
Cas No.:2406278-81-5
Sample solution is provided at 25 µL, 10mM.
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OM-153 is a potent and orally active tankyrase inhibitor with IC50s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM[1][2].
OM-153 shows picomolar IC50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable absorption, distribution, metabolism, and excretion (ADME) properties, and an improved pharmacokinetic profile in mice[1].
OM-153 decreases cell growth in COLO 320DM cells with a GI50 value of 10 nM and a GI25 value of 2.5 nM (concentrations resulting in 50% and 25% growth inhibition, respectively), while cell growth in RKO cells was insubstantially affected by the treatment[2].
OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines[2].
OM-153 (0.1-10 mg/kg; p.o.; twice daily; for 34 days) reduces WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts[2].
OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model[2].
| Animal Model: | CB17-SCID mice bearing COLO 320DM cells[2] |
| Dosage: | 10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg |
| Administration: | p.o.; twice daily; for 34 days |
| Result: | Reduced WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts. |
| Animal Model: | C57BL/6N mice injected with B16-F10 tumors[2] |
| Dosage: | 10 mg/kg, 1 mg/kg, and 0.1 mg/kg |
| Administration: | p.o.; twice daily; for 20 days |
| Result: | Potentiated anti-PD-1 immune checkpoint inhibition and antitumor effect. |
[1]. Leenders RGG, et al. Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II. J Med Chem. 2021;64(24):17936-17949.
[2]. Shoshy A. Brinch, et al. The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models. Cancer Research Communications (2022) 2 (4): 233-245.
| Cas No. | 2406278-81-5 | SDF | Download SDF |
| 分子式 | C28H24FN7O2 | 分子量 | 509.53 |
| 溶解度 | DMSO : 100 mg/mL (196.26 mM; Need ultrasonic) | 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 | 1.9626 mL | 9.813 mL | 19.6259 mL |
| 5 mM | 0.3925 mL | 1.9626 mL | 3.9252 mL |
| 10 mM | 0.1963 mL | 0.9813 mL | 1.9626 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet