Onvansertib NMS-1286937; NMS-P937|cas:1034616-18-6|西域试剂

Onvansertib NMS-1286937; NMS-P937,99.16%

产品编号：Bellancom-15828| CAS NO：1034616-18-6| 分子式：C₂₄H₂₇F₃N₈O₃| 分子量：532.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15828	￥650.00	杭州北京（现货）
Bellancom-15828	￥1000.00	杭州北京（现货）
Bellancom-15828	￥2600.00	杭州北京（现货）
Bellancom-15828	￥4900.00	杭州北京（现货）

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Onvansertib NMS-1286937; NMS-P937

产品介绍

nMS-1286937 是一种有效、高选择性、可口服的 PLK1 抑制剂，IC₅₀ 值为 2 nM。

生物活性

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC₅₀ of 2 nM.

体外研究

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with IC₅₀ of 2 nM. NMS-1286937 also shows inhibitory activities against FLT3, MELK, and CK2, with IC₅₀s of 510, 744, and 826 nM, respectively. NMS-P937 possesses a pure ATP competitive mechanism with a reversible dissociation and no time dependency. NMS-P937 (10 μM) is selective with a marginal activity of 48% and 40% inhibition on PLK2 and PLK3, respectively. NMS-P937 shows antiproliferative activity against a panel of 137 cell lines, with IC₅₀ values of below 100 nM for 60 of 137 cell lines and higher than 1 μM for only 9 of 137 cell lines. NMS-P937 shows cytotoxic activity against AmL-NS8 cells with IC₅₀ of 36 nM.

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

体内研究

NMS-1286937 (45 mg/kg, i.v.) shows a good tumor growth inhibition with acceptable and reversible body weight loss in CD1 nu/nu mice xenografted with human HCT116 colon adenocarcinoma cells. NMS-1286937 (60 mg/kg, p.o.) also inhibits the growth of tumor on HCT116 xenograft model. NMS-P937 (45 mg/kg, i.v.or 60 mg/kg, p.o) inhibits tumor growth to a comparable degree (TGI, 83% and 79% intravenously and orally, respectively) in HCT116-bearing mice. The combination of NMS-P937 (120 mg/kg given for 4 cycles of 2 consecutive days with 10-day rest) and cytarabine (75 mg/kg for 4 cycles of 5 consecutive days with 7-day rest) in the disseminated leukemia model AmL-PS is well tolerated and clearly showed increased mice survival. NMS-P937 (60 mg/kg bid os per day over 2 days with a 5 day rest) shows good efficacy compared to standard therapies, with a significant increase in median survival time (MST) in the established disease setting.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 21 mg/mL (39.44 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8779 mL	9.3893 mL	18.7786 mL
5 mM	0.3756 mL	1.8779 mL	3.7557 mL
10 mM	0.1878 mL	0.9389 mL	1.8779 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.76 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (3.76 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.76 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。