MKC8866
目录号 : KM2575 CAS No. : 1338934-59-0 纯度 : 98%

MKC8866 是一种水杨醛类似物,有效的选择性 IRE1 RNase 抑制剂,在体外的 IC50 为 0.29 μM。 MKC8866 强烈抑制 Dithiothreitol 诱导的 XBP1s 表达,EC50 为 0.52 μM。MKC8866 抑制无应激 RPMI 8226 细胞,IC50 为 0.14 μM。 MKC8866 抑制乳腺癌细胞中的 IRE1 RNase 导致促肿瘤发生因子减少,同时也能抑制前列腺癌 (PCa) 肿瘤的生长。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg 询价 In-stock
200mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.

体外研究

MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines.
MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase.
MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells.
MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s .

Cell Proliferation Assay

Cell Line: MCF7, SKBR3, MDA-MB-231 and MCF10A cells
Concentration: 20 μM
Incubation Time: For 6 days
Result: Decreased proliferation of all breast cancer cell lines.

Cell Cycle Analysis

Cell Line: MDA-MB-231, MCF7 and SKBR3 cells
Concentration: 20 μM
Incubation Time: 48 hours
Result: Reduced the number of cells entering S phase.

Cell Cycle Analysis

Cell Line: LNCaP, VCaP, 22Rv1 and C4-2B cells
Concentration: 0.2, 0.5, 1, 5, 10 μM
Incubation Time: 3 days
Result: Suppressed the viability of all four cell lines in a dose-dependent manner.

Cell Cycle Analysis

Cell Line: MDA-MB-231 cells
Concentration: 20 μM
Incubation Time: 72  hours
Result: Completely blocked NSC 125973-induced expression of XBP1s.
体内研究

MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal.

Animal Model: Female athymic nude mice with MDA-MB-231 tumor
Dosage: 300 mg/kg
Administration: Oral; for 28 days
Result: Reduced tumor regrowth post-NSC 125973 withdrawal.
分子式
C18H19NO7
分子量
361.35
CAS号
1338934-59-0
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 : 16.67 mg/mL (46.13 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7674 mL 13.8370 mL 27.6740 mL
5 mM 0.5535 mL 2.7674 mL 5.5348 mL
10 mM 0.2767 mL 1.3837 mL 2.7674 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: ≥ 1.67 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 1.67 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 16.7 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 1.67 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 16.7 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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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