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^[1]. LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research^[1].

EC50: 3.2 μM (tubulin polymerization)^[1]

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^[1].
LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC₅₀ value of LP-261 is 5.0 μM^[1]. 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^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
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^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

421.47

C₂₂H₁₉N₃O₄S

915412-67-8

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

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

*

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。

• [1]. Rupa S Shetty, et al. Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. J Med Chem. 2011 Jan 13;54(1):179-200