OM-153|cas:2406278-81-5|西域试剂

OM-153,99.59%

产品编号：Bellancom-145267| CAS NO：2406278-81-5| 分子式：C₂₈H₂₄FN₇O₂| 分子量：509.53

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-145267		￥5800.00	杭州北京（现货）
Bellancom-145267		￥9800.00	杭州北京（现货）

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OM-153

产品介绍

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 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.

体外研究

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.
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.
OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CB17-SCID mice bearing COLO 320DM cells
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
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CB17-SCID mice bearing COLO 320DM cells
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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (196.26 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-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。

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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。