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CAS No.: 1037184-44-3

YK-4-279 Catalog No. CSN16911

Synonyms: YK-4-279

YK 4-279 is a potent inhibitor of RNA Helicase A (RHA) that binding to the oncogenic transciption factor EWS-FLI1.

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400-920-2911

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技术信息

生物活性

描述The erythroblastosis virus E26 transforming sequences (ETS) family of transcription factors consists of a highly conserved group of genes that play important roles in cellular proliferation, differentiation, migration and invasion. ERG and ETV1 are the most commonly translocated ETS proteins, YK-4-279 is a small molecule antagonist of ETV1^[3]. Due to its hydrophobic structure, the bioavailability of YK-4-279 is only 2%-15% when it is administered to mice by oral gavage. Intra-peritoneal administrations of 75 mg/kg YK-4-279 initially leads to a steep rise in plasma concentrations, but is substantially cleared leading to ,1 mM levels by 2 hours^[4]. Exposure of LNCaP-luc-M6 cells to 1 mM YK-4-279 resulted in significantly reduced mRNA levels of several ETV1 target genes, including MMP7, MMP13, FKBP10 and GLYATL2, without affecting the expression of ETV1^[3]. Maximal YK-4-279 concentrations (Cmax) of 90 and 10 μmol/L, respectively, occurred 30 minutes after i.p. or p.o. dosing. YKPO achieved an oral bioavailability of 61% to 73% and peak serum concentration 6.7-fold higher than the half-maximal inhibitory dose observed in vitro (IC50, 1 μmol/L)^[5]. The combination of low-dose docetaxel and YK-4-279 synergistically inhibited growth and induced apoptosis in human prostate cancer cells. The combination also more efficiently suppressed the migration and invasion of LNCaP and PC-3 cells. The combination of low-dose docetaxel and YK-4-279 caused a stronger decrease in the levels of ETV1, AR, PSA, p-STAT3,survivin, Bcl-2, and p-Akt in LNCaP cells and of p-Akt, Bcl-2, and p-STAT3 in PC-3 cells compared with either drug alone^[6].
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
- 2.7308 mL
- 13.6539 mL
- 27.3078 mL
- 5 mM
- 0.5462 mL
- 2.7308 mL
- 5.4616 mL
- 10 mM
- 0.2731 mL
- 1.3654 mL
- 2.7308 mL

技术信息

CAS号

1037184-44-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H13Cl2NO4

运输

蓝冰

分子量

366.20

别名

YK-4-279

溶解度

DMSO	73.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (136.5 mM) warming

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