LP-261|cas:915412-67-8|西域试剂

LP-261,99.77%

产品编号：Bellancom-14389| CAS NO：915412-67-8| 分子式：C₂₂H₁₉N₃O₄S| 分子量：421.47

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-14389	￥900.00	杭州北京（现货）
Bellancom-14389	￥1500.00	杭州北京（现货）
Bellancom-14389	￥2500.00	杭州北京（现货）
Bellancom-14389	￥4500.00	杭州北京（现货）
Bellancom-14389	￥7500.00	杭州北京（现货）

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LP-261

产品介绍

LP-261 是一种有效的具有口服活性的抗有丝分裂剂 (antimitotic agent)，对体外微管蛋白聚合有抑制作用，其 EC₅₀ 为 3.2 μM。LP-261 在体内可抑制人非小细胞肺癌 (NCI-H522) 的生长，可用于癌症研究。

生物活性

LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC₅₀ of 3.2 μM. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research.

体外研究

LP-261 shows potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01μM to 0.38 μM across the tested cell lines, the IC₅₀ values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 values are 0.01 μM, 0.01 μM, 0.02 μM, 0.05 μM, 0.05μM and 0.07 μM, respectively.
LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC₅₀ value of LP-261 is 5.0 μM. LP-261 has the ability to compete with colchicine for binding to tubulin in a [³H]colchicine competition binding assay, the EC₅₀ (3.2 μM) for LP-261 to inhibit the binding with a potency similar to that of colchicine itself, and it exhibits a 79% inhibition at a conctration of 30 μM.

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

体内研究

LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (T_max=2.0 h), the terminal half-life of 1.4 h ( 0.2 h indicated a moderate rate of elimination in rat, and the volume of distribution (V_ss) is 1.25 L/kg.
LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm³ versus 3769 mm³ in the vehicle treated group, this represents a 96% reduction in mean tumor volume. Meanwhile, LP-261 at 15 mg/kg leads to a 41% inhibition after 28 days in this mouse model.

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

Animal Model:	Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice
Dosage:	15 or 50 mg/kg
Administration:	Oral gavage; 15 or 50 mg/kg; twice daily; 28 days
Result:	Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights.

体内研究

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

Animal Model:	Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice
Dosage:	15 or 50 mg/kg
Administration:	Oral gavage; 15 or 50 mg/kg; twice daily; 28 days
Result:	Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (79.08 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3726 mL	11.8632 mL	23.7265 mL
5 mM	0.4745 mL	2.3726 mL	4.7453 mL
10 mM	0.2373 mL	1.1863 mL	2.3726 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 (5.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.93 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.93 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。