OM-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。
| 生物活性 | OM-153 is a potent and orally activetankyraseinhibitor withIC50s of 13 nM and 2 nM fortankyrase 1andtankyrase 2(TNKS1/2), respectively. OM-153 inhibits luciferase-basedWnt/β-cateninsignaling reporter activity with anIC50value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM[1][2]. |
| IC50& Target[1][2] | TNKS1 13 nM (IC50) | TNKS2 2 nM (IC50) | Wnt/β-catenin 0.63 nM (IC50) |
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体外研究
(In Vitro) | OM-153 shows picomolar IC50inhibition (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 GI50value of 10 nM and a GI25value 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].
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体内研究
(In Vivo) | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(196.26 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9626 mL | 9.8130 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 |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.91 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.91 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.91 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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