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CCF642 

目录号: HY-100430 纯度: ≥98.0%
产品使用指南

CCF642 是一种有效的蛋白质二硫键异构酶 (PDI) 抑制剂,IC50 为 2.9 μM。CCF642 在多发性骨髓瘤细胞中引起急性内质网 (ER) 应激,并伴随凋亡诱导的钙释放。CCF642 具有广泛的抗多发性骨髓瘤活性。

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CCF642 Chemical Structure

CCF642 Chemical Structure

CAS No. : 346640-08-2

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规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥749
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2 mg ¥500
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5 mg ¥900
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10 mg ¥1250
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25 mg ¥2500
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50 mg ¥4500
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100 mg ¥6500
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  • 生物活性

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  • 参考文献

生物活性

CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity[1].

IC50 & Target

IC50: 2.9 μM (PDI)[1]

体外研究
(In Vitro)

CCF642 (3 μM; 0.5-6 hours) increases PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins[1].
CCF642, a bone marrow-sparing compound, exhibits a submicromolar IC50 in 10 of 10 multiple myeloma cell lines (MM1.S, MM1.R, KMS-12-PE, KMS-12-BM, NCI-H929, U266, RPMI 8226, JJN-3, HRMM.09-luc, 5TGM1-luc)[1].

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

Western Blot Analysis[1]

Cell Line: MM1.S cells
Concentration: 3 μM
Incubation Time: 0.5, 1, 2, 4, 6 hours
Result: Increased PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins.
体内研究
(In Vivo)

CCF642 (10 mg/kg; i.p.; three times a week; for 24 days) significantly prolongs life of 5TGM1-luc-bearing mice and suppresses 5TGM1-luc growth as determined by life imaging[1].

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

Animal Model: C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc[1]
Dosage: 10 mg/kg
Administration: i.p.; three times a week; for 24 days
Result: Significantly prolonged life of 5TGM1-luc–bearing mice and suppressed 5TGM1-luc growth as determined by life imaging.
分子量

378.45

Formula

C15H10N2O4S3

CAS 号
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 : ≥ 30 mg/mL (79.27 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6424 mL 13.2118 mL 26.4236 mL
5 mM 0.5285 mL 2.6424 mL 5.2847 mL
10 mM 0.2642 mL 1.3212 mL 2.6424 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: 0.62 mg/mL (1.64 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.62 mg/mL (1.64 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 6.2 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
*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
CCF642
目录号:
HY-100430
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