CCF642 - CAS:346640-08-2

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CCF642

目录号 : KM3745 CAS No. : 346640-08-2 纯度 : ≥98%

Data Sheet 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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2mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

体外研究

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.
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).

Western Blot Analysis

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

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.

Animal Model:	C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc
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.

分子式

C₁₅H₁₀N₂O₄S₃

分子量

378.45

CAS号

346640-08-2

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。