OTS514|cas:1338540-63-8|西域试剂

OTS514,98.15%

产品编号：Bellancom-18621| CAS NO：1338540-63-8| 分子式：C₂₁H₂₀N₂O₂S| 分子量：364.46

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货号	价格	库存与货期
Bellancom-18621	￥1100.00	杭州北京（现货）
Bellancom-18621	￥2000.00	杭州北京（现货）
Bellancom-18621	￥3500.00	杭州北京（现货）
Bellancom-18621	￥7000.00	杭州北京（现货）
Bellancom-18621	￥11000.00	杭州北京（现货）

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OTS514

产品介绍

OTS5144 是一种高效的 TOPK 抑制剂，IC₅₀ 为 2.6 nM。OTS514 强效抑制 TOPK 阳性的肿瘤细胞生长。OTS514 诱导细胞周期停滞和凋亡 (apoptosis)。

生物活性

OTS514 is a highly potent TOPK inhibitor with an IC₅₀ of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.

体外研究

OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138⁺ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells.

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

Cell Viability Assay

Cell Line:	Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
Concentration:	1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
Incubation Time:	72 hours
Result:	IC₅₀ values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, is resistant.

体内研究
(In Vivo)

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells).

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

Animal Model:	Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells
Dosage:	1, 2.5, and 5 mg/kg
Administration:	Intravenously treated; once every day for 2 weeks
Result:	Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.

体内研究

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells).

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

Animal Model:	Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells
Dosage:	1, 2.5, and 5 mg/kg
Administration:	Intravenously treated; once every day for 2 weeks
Result:	Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.

体内研究

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells).

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

Animal Model:	Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells
Dosage:	1, 2.5, and 5 mg/kg
Administration:	Intravenously treated; once every day for 2 weeks
Result:	Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (274.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7438 mL	13.7189 mL	27.4379 mL
5 mM	0.5488 mL	2.7438 mL	5.4876 mL
10 mM	0.2744 mL	1.3719 mL	2.7438 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: ≥ 2.5 mg/mL (6.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.86 mM，饱和度未知) 的澄清溶液。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.86 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。