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CAS No.: 1431280-51-1

VLX1570 Catalog No. CSN13933

Synonyms: VLX1570

VLX1570 is a deubiquitinylating enzyme DUB competitive inhibitor with an IC50 of approximately 10 μM in vitro and shows coinhibition of the deubiquitinating enzymes, like USP14 and UCHL5.

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技术信息

生物活性

描述Deubiquitinating enzymes (DUBs) are key components of the ubiquitin-dependent protein degradation pathway and act as master regulators in a number of metabolic processes including cell growth, differentiation, and apoptosis^[3]. VLX1570 is a competitive inhibitor of proteasome DUB activity with IC50 value of 10 μM. In vitro, VLX1570 induced the accumulation of proteasome-bound high molecular weight polyubiquitin conjugates and an apoptotic response. Inhibition of USP14 activity could be demonstrated in cells exposed to 0.5 μM VLX1570 whereas UCHL5 inhibition was weak in comparison. VLX1570 inhibited multiple myeloma cells proliferation, including KMS-11, RPMI8226, OPM-2 and OPM-2-BZ^R cell lines, with IC50 values ranging in 43 – 191 nM^[4]. In addition, VLX1570 inhibited cell viability of ALL cell lines including 697, Reh, SEM, RS4;11, SUP-B15, CCRF-CEM and T-ALL cell lines, with IC50 values ranging in 50 - 100 nM, suggesting its highly sensitive to acute lymphoblastic leukemia cells^[5]. In vivo, administered VLX1570 at 4.0 mg/kg via intraperitoneal injection every alternate day for 20 days resulted in decreased tumor burden and prolonged survival in waldenstrom macroglobulinemia tumor xenografted mice^[6]. Treatment of a xenograft mouse model of ewing sarcoma (EWS) with VLX1570 at dose of 4.4 mg/kg once daily via intraperitoneal administration for 2 weeks significantly inhibited in vivo tumor growth^[7].
作用机制VLX1570 interferes with the proteasomal degradation by inhibiting the activities of the proteasomal DUBs USP14 and UCHL5^[5].
动物研究
剂量
Mice: 3 mg/kg^[2] (i.v.); 4.4 mg/kg^[2] (i.p.)

给药途径
i.v., i.p.
临床研究

动物研究
剂量	Mice: 3 mg/kg^[2] (i.v.); 4.4 mg/kg^[2] (i.p.)
给药途径	i.v., i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02372240	Multiple Myeloma	Phase 1 Phase 2	Terminated(Dose limiting tox i... more >>s observed. Study put on full clinical hold.) Collapse <<	-	United States, New York ... more >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1304 mL
- 10.6520 mL
- 21.3040 mL
- 5 mM
- 0.4261 mL
- 2.1304 mL
- 4.2608 mL
- 10 mM
- 0.2130 mL
- 1.0652 mL
- 2.1304 mL

技术信息

CAS号

1431280-51-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H17F2N3O6

运输

蓝冰

分子量

469.39

别名

VLX1570

溶解度

DMSO	93.0 mg/mL (198.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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