标签归档：lanreotide

Lanreotide acetate(Synonyms: BIM 23014 acetate)

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Lanreotide acetate;(Synonyms: BIM 23014 acetate) 纯度: 99.91%

Lanreotide acetate (BIM 23014 acetate) 是一种具有抗肿瘤活性的生长抑素类似物。Lanreotide acetate 可用于类癌综合症。

Lanreotide acetateamp;;(Synonyms: BIM 23014 acetate)

Lanreotide acetate Chemical Structure

CAS No. : 2378114-72-6

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥1650 In-stock
5 mg ￥750 In-stock
10 mg ￥1300 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

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生物活性

Lanreotide acetate (BIM 23014 acetate) is a somatostatin analogue with antineoplastic activity. Lanreotide acetate can be used for carcinoid syndrome[1][2].

体外研究
(In Vitro)

Lanreotide acetate (BIM 23014 acetate) (24-48 hours; 100  nM; GH3 cells) combines with radiation increasing in apoptotic sub-G1 proportion[1].
Lanreotide acetate results in a dose-dependent decrease in GH3 cell colony forming units. Lanreotide acetate at doses of 1, 10, 100, and 1000 nM results in cell survival rates of 75, 56, 39 and 27% respectively. The IC50 (50% inhibition of cell growth) was 57 nM[1].
Lanreotide acetate inhibits GH-secreting pituitary adenoma cell proliferation and hormone release in vitro[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Lanreotide acetate (2.5-10mg/kg; s.c.; daily for 5 days) resluts in tumor growth inhibition[1].

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

Animal Model: Male nude mice, 8 weeks old and 20–25 g in body weight (GH3 tumor-bearing nude mice)[1]
Dosage:  2.5, 5, 10 mg/kg
Administration: Subcutaneous; daily for 5 days
Result: Produced tumor growth inhibition.

Clinical Trial

分子量

1156.38

Formula

C56H73N11O12S2
CAS 号

2378114-72-6
Sequence

{d-2nal}-Cys-Tyr-{d-Trp}-Lys-Val-Cys-Thr-NH2 (Disulfide bridge: Cys2-Cys7)
Sequence Shortening

{d-2nal}-CY-{d-Trp}-KVCT-NH2 (Disulfide bridge: Cys2-Cys7)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (86.48 mM; Need ultrasonic)

H2O : 25 mg/mL (21.62 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8648 mL 4.3238 mL 8.6477 mL
5 mM 0.1730 mL 0.8648 mL 1.7295 mL
10 mM 0.0865 mL 0.4324 mL 0.8648 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 (protect from light, 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 (2.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.16 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 (2.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.16 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 (2.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.16 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 MCE 网站选购。
参考文献

  • [1]. Ning S, et al. Lanreotide promotes apoptosis and is not radioprotective in GH3 cells.Endocr Relat Cancer. 2009 Sep;16(3):1045-55.

    [2]. Florio T, et al. Characterization of the intracellular mechanisms mediating somatostatin and lanreotide inhibition of DNA synthesis and growth hormone release from dispersed human GH-secreting pituitary adenoma cells in vitro.Clin Endocrinol (Oxf). 2003 Jul;59(1):115-28.