CCF642

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。

CAS号

346640-08-2

分子式

C15H10N2O4S3

主要靶点

Others

仅限科研使用

Cat No : CM06639

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Synonyms

AC1LYELL



产品信息

CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.

CAS号 346640-08-2
分子式 C15H10N2O4S3
主要靶点 Others
主要通路 其他
分子量 378.45
纯度 97.12%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 AC1LYELL

靶点活性

PDI:2.9 μmol/L

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].

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].

溶解度

DMSO:7.6 mg/mL (20 mM)

参考文献

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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