Leptomycin B 来普霉素B; CI 940; LMB|cas:87081-35-4|西域试剂

Leptomycin B 来普霉素B; CI 940; LMB,99.54%

产品编号：Bellancom-16909| CAS NO：87081-35-4| 分子式：C₃₃H₄₈O₆| 分子量：540.73

Leptomycin B (CI 940; LMB) 是一种蛋白出核转运抑制剂。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1/exportin 1 失活。 Leptomycin B 是一种有效的抗真菌抗生素，可阻断真核细胞周期。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-16909		￥3800.00	杭州北京（现货）
Bellancom-16909		￥12800.00	杭州北京（现货）

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Leptomycin B 来普霉素B; CI 940; LMB

产品介绍

Leptomycin B (CI 940; LMB) 是一种蛋白出核转运抑制剂。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1/exportin 1 失活。 Leptomycin B 是一种有效的抗真菌抗生素，可阻断真核细胞周期。

生物活性

Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.

体外研究

Leptomycin B (LMB) is very potent in vitro against various cancer cell lines (IC50 values in the 0.1 to 10 nM range). Leptomycin B (LMB) inhibits SiHa, HCT-116, and SKNSH cells with IC₅₀s of 0.4, 0.3 and 0.4 nM for a 72 hour exposure, respectively.
Leptomycin B (LMB) (0.5 nM) displays a synergistic effect on Gefitinib (0–32 μM)-induced cytotoxicity in A549 and H460 cell line. The simultaneous treatments of Gefitinib (0–32 μM) and Leptomycin B (0.5 nM) show synergistic cytotoxic effect on A549 as compared to Gefitinib alone at both 24 and 48 hours.

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

Cell Viability Assay

Cell Line:	The non-small cell lung cancer (NSCLC) cell lines A549 and H460
Concentration:	0.5 nM
Incubation Time:	24 and 48 hours
Result:	The IC₅₀ of Gefitinib at 48 hours was 32.0±2.5 μM while it was significantly reduced to 25.0±2.1 μM with the combination of 0.5 nM Leptomycin B. The significant synergistic cytotoxic effect from co-treatment of 0.5 nM Leptomycin B with Gefitinib was also confirmed in H460 cell line.

Cell Viability Assay

Cell Line:	A549
Concentration:	0.5 nM
Incubation Time:	48 hours
Result:	0.5 nM Leptomycin B plus Gefitinib or Gefitinib alone had a decreased p-EGFR(Tyr1068) expressions compared with controls. p-Akt (Ser473) was inhibited in a dose-response manner by Gefitinib treatments, but it was enhanced by gefitinib+Leptomycin B co-treatments compared with gefitinib alone. A549 treated by Gefitinib+Leptomycin B had a higher expression of p-Erk1/2(Thr202/Tyr204) than A549 treated by Gefitinib alone.

体内研究
(In Vivo)

Leptomycin B (LMB) is poorly tolerated in vivo. Maximum tolerated dose (MTD) is 2.5 mg/kg for LMB (single i.v.) in HCT-116 tumor–bearing mice.The limited in vivo efficacy of Leptomycin B is due to off-target effects because our nuclear export inhibitors (NEIs) retain the potent inhibition of CRM1, but are clearly better tolerated in vivo^[4].

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.

体内研究

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

性状

<41°C Solid,>44°C Liquid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (184.94 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8494 mL	9.2468 mL	18.4935 mL
5 mM	0.3699 mL	1.8494 mL	3.6987 mL
10 mM	0.1849 mL	0.9247 mL	1.8494 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 (stored under nitrogen)。-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 (4.62 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.62 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 (4.62 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.62 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.62 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。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

参考文献

. N Kudo, et al. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue in the central conserved region. Proc Natl Acad Sci U S A. 1999 Aug 3;96(16):9112-7. [Content Brief]

. Sarah C Mutka,et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Res. 2009 Jan 15;69(2):510-7. [Content Brief]

. Zhongwei Liu, et al.Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. [Content Brief]

[4]. Sarah C Mutka, et al. Identification of nuclear export inhibitors with potent anticancer activity in vivo. Cancer Res. 2009 Jan 15;69(2):510-7. [Content Brief]

化学品安全说明书(MSDS)

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产品编号(Item Number)

批号(Lot Number)

符号	GHS02, GHS06, GHS08
信号词	Danger
危害声明	H225-H301-H311-H331-H370
警示性声明	P210-P260-P280-P301 + P310-P311
危害码 (欧洲)	T: Toxic;F: Flammable;
风险声明 (欧洲)	R23/25
安全声明 (欧洲)	7-16-24-33-45
危险品运输编码	UN 1230 3
WGK德国	3
海关编码	2916190090

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Leptomycin B 来普霉素B; CI 940; LMB,99.54%

Leptomycin B 来普霉素B; CI 940; LMB

化学品安全说明书(MSDS)

质检证书(COA)

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