Melflufen hydrochloride Melphalan flufenamide hydrochloride,99.20%

产品编号:Bellancom-105019A| CAS NO:380449-54-7| 分子式:C24H31Cl3FN3O3| 分子量:534.88

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-105019A
4200.00 杭州 北京(现货)
Bellancom-105019A
7000.00 杭州 北京(现货)
Bellancom-105019A
19000.00 杭州 北京(现货)
Bellancom-105019A
29000.00 杭州 北京(现货)

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Melflufen hydrochloride Melphalan flufenamide hydrochloride

产品介绍 Melflufen (Melphalan flufenamide) hydrochloride,Melphalan 的一种二肽前体活性分子,是一种烷基化剂。Melflufen hydrochloride 对多发性骨髓瘤细胞具有抗肿瘤活性,并抑制血管生成。Melflufen hydrochloride 对骨髓瘤细胞 DNA 不可逆损伤及细胞毒作用。
生物活性

Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.

体外研究

Melflufen (Melphalan flufenamide) hydrochloride (0.5-10 μM; 24 hours) decreases viability of MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, and ANBL-6 cells in a concentration-dependent manner.
Melflufen hydrochloride induces apoptosis in MM.1S cells.
Melflufen hydrochloride also is a potent activator of exosome secretion.

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

Cell Viability Assay

Cell Line: Multiple myeloma cells: MM.1S, INA-6, RPMI-8226, MM.1R, Dox-40, ARP-1, ANBL-6 cells
Concentration: 0.5, 1, 3, 5, 10 μM
Incubation Time: 24 hours
Result: A significant concentration-dependent decrease in viability of all cell lines was observed.
体内研究
(In Vivo)

Melflufen (Melphalan flufenamide) hydrochloride (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model.

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

Animal Model: CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)
Dosage: 3 mg/kg
Administration: 1.v.; twice-weekly for two weeks
Result: Significantly inhibited MM tumor growth and prolonged survival of mice.
体内研究

Melflufen (Melphalan flufenamide) hydrochloride (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model.

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

Animal Model: CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)
Dosage: 3 mg/kg
Administration: 1.v.; twice-weekly for two weeks
Result: Significantly inhibited MM tumor growth and prolonged survival of mice.
体内研究

Melflufen (Melphalan flufenamide) hydrochloride (3 mg/kg; i.v.; twice-weekly for two weeks) shows anti-MM activity in xenograft mouse model.

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

Animal Model: CB-17 SCID mice (human plasmacytoma MM.1S xenograft mouse model)
Dosage: 3 mg/kg
Administration: 1.v.; twice-weekly for two weeks
Result: Significantly inhibited MM tumor growth and prolonged survival of mice.
性状Solid
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (62.31 mM; Need ultrasonic)

H2O : 1 mg/mL (1.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8696 mL 9.3479 mL 18.6958 mL
5 mM 0.3739 mL 1.8696 mL 3.7392 mL
10 mM 0.1870 mL 0.9348 mL 1.8696 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 (sealed storage, away from moisture)。-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 (4.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.67 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 (4.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.67 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 (4.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.67 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。

  • 4.

    请依序添加每种溶剂: PBS

    Solubility: 1 mg/mL (1.87 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

*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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

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