CAS |
No.1037184-44-3 |
英文名称 |
YK-4-279 |
别名 |
;YK4-279;CS-0667; |
分子式 |
C17H13Cl2NO4 |
分子量 |
366.2 |
溶解性 |
Soluble in DMSO |
纯度 |
≥98% |
外观(性状) |
White to off-white Solid |
储存条件 |
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
MDL |
MFCD18382120 |
SMILES |
ClC1=C2C(C(O)(CC(C3=CC=C(OC)C=C3)=O)C(N2)=O)=C(Cl)C=C1 |
靶点 |
DNA/RNA Synthesis |
通路 |
Cell Cycle;DNA Damage/DNA Repair |
背景说明 |
YK-4-279是EWS-FLI1与RNA helicase A (RHA)结合的有效抑制剂。 |
生物活性 |
YK-4-279 blocks RNA Helicase A (RHA) binding with EWS-FLI1 (oncogenic protein). YK-4-279 induces apoptosis and shows anti-proliferation activities towards various cancer cells. YK-4-279 has a chiral center and it can be separated into two enantiomers. YK-4-279 can be used for the research of cancer[1-2]. |
In Vitro |
YK-4-279, a derivative of the lead compound from the screen, blocks RHA binding to EWS-FLI1, induces Apoptosis in ESFT cells and reduces the growth of ESFT orthotopic xenografts.[1].YK-4-279 (0.1-30 μM; 72 h) inhibits the growth of ESFT, prostate, breast and pancreatic cancer cells[2]. |
In Vivo |
YK-4-279 (1.5 mg; i.p. once) inhibited ESFT tumor growth[1]. |
数据来源文献 |
[1]. Erkizan HV, et al. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewings sarcoma. Nat Med. 2009 Jul;15(7):750-6.
[2]. Barber-Rotenberg JS, et al. Single enantiomer of YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1. Oncotarget. 2012 Feb;3(2):172-82. |
规格 |
1mg 5mg 10mg 25mg 50mg 100mg 200mg |
单位 |
瓶 |