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CCF642

产品编号 T6800 CAS 346640-08-2

别名: AC1LYELL

CCF642 (AC1LYELL) 是蛋白质二硫键异构酶抑制剂(IC50:2.9 μM)。它在多发性骨髓瘤细胞中引起急性内质网应激，并伴随凋亡诱导的钙释放，表现出广泛的抗多发性骨髓瘤作用。

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CCF642, CAS 346640-08-2

规格	价格/CNY	货期
1 mg	￥ 289	现货
2 mg	￥ 413	现货
5 mg	￥ 747	现货
10 mg	￥ 987	现货
25 mg	￥ 1,980	现货
50 mg	￥ 3,710	现货
100 mg	￥ 5,330	现货
500 mg	￥ 10,900	待询
1 mL * 10 mM (in DMSO)	￥ 619	现货

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纯度: 97.12%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	CCF642 (AC1LYELL) is a novel PDI-inhibiting compound with antimyeloma activity.
靶点活性	PDI:2.9 μmol/L
体外活性	In vitro, CCF642 inhibits PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. Computational modeling suggests a novel covalent binding mode in active-site CGHCK motifs. CCF642 causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release[1].
体内活性	CCF642 displays potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolongs the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib[1].
激酶实验	Inhibition of CB-839 on rHu-GAC: The enzymatic activity is measured in assay buffer containing 50 mM Tris-Acetate pH 8.6, 150 mM K2HPO4 , 0.25 mM EDTA, 0.1 mg/mL bovine serum albumin, 1 mM DTT, 2 mM NADP+ and 0.01% Triton X-100. To measure inhibition, the inhibitor (prepared in DMSO) is first pre-mixed with glutamine and glutamate dehydrogenase (GDH) and reactions are initiated by the addition of rHu-GAC. Final reactions contains 2 nM rHu-GAC, 10 mM glutamine, 6 units/mL GDH and 2% DMSO. Generation of NADPH is monitored by fluorescence (Ex340/Em460 nm) every minute for 15 minutes on a SpectraMax M5e plate reader. Relative fluorescence units (RFU) are converted to units of NADPH concentration (μM) using a standard curve of NADPH. Each assay plate incorporates control reactions that monitores the conversion of glutamate (1 to 75 μM) plus NADP+ to α-ketoglutarate plus NADPH by GDH. Under these assay conditions, up to 75 μM glutamate is stoichiometrically converts to α-ketoglutarate/NADPH by GDH. Initial reaction velocities are calculated by fitting the first 5 minutes of each progress curve to a straight line. Inhibition curves are fitted to a four-parameter dose response equation of the form: % activity = Bottom + (Top-Bottom)/(1+10^((LogIC50-X)*HillSlope)).

别名	AC1LYELL
分子量	378.45
分子式	C15H10N2O4S3
CAS No.	346640-08-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 7.6 mg/mL (20 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6424 mL	13.2118 mL	26.4236 mL	66.0589 mL
	5 mM	0.5285 mL	2.6424 mL	5.2847 mL	13.2118 mL
	10 mM	0.2642 mL	1.3212 mL	2.6424 mL	6.6059 mL
	20 mM	0.1321 mL	0.6606 mL	1.3212 mL	3.3029 mL

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参考文献

1. Vatolin S, et al. Cancer Res. 2016, 76(11):3340-50.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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