1. Metabolic Enzyme/Protease
    Autophagy
  2. Proteasome
    Autophagy
  3. Ixazomib citrate

Ixazomib citrate (Synonyms: 枸橼酸艾沙佐米; MLN9708)

目录号: HY-10452 纯度: 99.89%
产品使用指南

Ixazomib citrate (MLN9708) 是 20S蛋白酶体胰凝乳蛋白酶样蛋白水解β5位点的可逆抑制剂,IC50 为3.4 nM和Ki为0.93 nM。

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Ixazomib citrate Chemical Structure

Ixazomib citrate Chemical Structure

CAS No. : 1239908-20-3

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10 mM * 1 mL in DMSO ¥570
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5 mg ¥500
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50 mg ¥1500
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.

IC50 & Target

IC50: 3.4 nM (20S proteasome β5), 31 nM (20S proteasome β1), 3500 nM (20S proteasome β2)[3]

体外研究
(In Vitro)

Ixazomib citrate (MLN9708; 0.20-3.20 µM) inhibits the cell growth of both cell lines effectively in a time- and dose-dependent manner. Ixazomib induces cell cycle arrest in MG-63 and Saos-2 cells. Ixazomib induces apoptosis mainly through the caspases pathway and requires the activation of both caspase8 and caspase9. Ixazomib treatment increases the levels of pro-apoptotic proteins and down regulates the anti-apoptotic proteins that control MOMP. Ixazomib treatment induces the release of Cytc, Smac, OMI from mitochondria and decreases the protein levels of XIAP. Ixazomib inhibits the invasion ability of MG-63 and Saos-2 cells and decreases both the expression and secretion levels of MMP2/9[1].Ixazomib citrate (MLN9708; 12 nM) shows inhibitory activity against C-L and T-L proteasome activities. Treatment of H929 and MM.1S MM cells with Ixazomib triggers a marked increase in proteolytic cleavage of poly(ADP) ribose polymerase (PARP), a signature event during apoptosis. Ixazomib induces cleavage of caspase-3, an upstream activator of PARP. Ixazomib induces eIf2-α kinase activity and protein levels of Bip and CHOP/GADD153. Ixazomib blocks BMSCs-induced MM cell proliferation, inhibits in vitro capillary tubule formation, and target NF-κB[2].

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

体内研究
(In Vivo)

Ixazomib citrate (MLN9708; 11 mg/kg) significantly inhibits MM tumor growth and prolongs survival in the human plasmacytoma MM.1S xenograft mouse model. The blood chemistry profiles of Ixazomib-treated mice show normal levels of creatinine, hemoglobin, and bilirubin. Ixazomib dramatically increases the number of cleaved-caspase-3 positive cells of the xenograft model[2].

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

Clinical Trial
分子量

517.12

Formula

C20H23BCl2N2O9

CAS 号
中文名称

枸橼酸艾沙佐米

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (483.45 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9338 mL 9.6689 mL 19.3379 mL
5 mM 0.3868 mL 1.9338 mL 3.8676 mL
10 mM 0.1934 mL 0.9669 mL 1.9338 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.02 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 20.8 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
Cell Assay
[1]

Cell viability is assessed using the MTT assay. Cells are trypsinized and seeded in 96-well plate at 5000 cells per well. Cells are treated with Ixazomib or DMSO in basal medium at the indicated doses and times. Cell viability is determined relative to control cells treated with vehicle alone.

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

Animal Administration
[2]

Ixazomib is dissolved in 5% 2-hydroxypropyl-β- cyclodextrin at 2 mg/mL concentration. The human plasmacytoma xenograft tumor model is used in the assay. CB-17 SCID mice (n=21) are subcutaneously inoculated with 5.0×106 MM.1S cells in 100 µL serum-free RPMI-1640 medium, and randomized to treatment groups when tumors reach 250-300 mm3. Mice are treated with vehicle, bortezomib (1 mg/kg; i.v) or Ixazomib (11 mg/kg; i.v) twice weekly for 3 weeks. Animals are euthanized when their tumors reach 2 cm3.

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

参考文献

纯度: 99.89%

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× = ×
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