YK-4-279

目录号: PL04055 纯度: ≥99%
YK-4-279 能够阻断 RNA 解旋酶 A (RHA) 与 EWS-FLI1 (致癌蛋白) 的结合。YK-4-279 诱导细胞凋亡并且对多种癌细胞具有抗增殖活性。YK-4-279 有一个手性中心并且可以被分离成两个对映体。YK-4-279 可用于癌症的研究。
CAS No. :1037184-44-3
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PL04055-10mg 10mg ¥607.00 请登录
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PL04055-100mg 100mg ¥3175.00 请登录
PL04055-200mg 200mg ¥4475.00 请登录
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PL04055-1 mL x 10 mM (in DMSO) 1 mL x 10 mM (in DMSO) ¥305.00 请登录
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中文名称
YK-4-279
中文别名
4,7-二氯-1,3-二氢-3-羟基-3-[2-(4-甲氧基苯基)-2-氧代乙基]-2H-吲哚-2-酮;YK-4-279 抑制剂
英文名称
YK-4-279
英文别名
4-Piperidinecarboxamide, N-[4-(6-methyl-2-benzothiazolyl)phenyl]-1-(2-thienylsulfonyl)-;YK-4-279;YK 4-279;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one YK-4-279;4,7-dichloro-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)indolin-2-one;C17H13Cl2NO4;4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one;MLS006010813;HMS3741G19;BCP13213;AOB87740;BDBM50379275;s7679;ABP000316;SMR0047
Cas No.
1037184-44-3
分子式
C17H13Cl2NO4
分子量
366.20
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述

YK-4-279 能够阻断 RNA 解旋酶 A (RHA) 与 EWS-FLI1 (致癌蛋白) 的结合。YK-4-279 诱导细胞凋亡并且对多种癌细胞具有抗增殖活性。YK-4-279 有一个手性中心并且可以被分离成两个对映体。YK-4-279 可用于癌症的研究。

产品详情
YK-4-279 能够阻断 RNA 解旋酶 A (RHA) 与 EWS-FLI1 (致癌蛋白) 的结合。YK-4-279 诱导细胞凋亡并且对多种癌细胞具有抗增殖活性。YK-4-279 有一个手性中心并且可以被分离成两个对映体。YK-4-279 可用于癌症的研究。
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.
性状
Solid
IC50 & Target[1][2]
IC50: 0.94 μM (TC32), 1.83 μM (TC71), 1.03 μM (RDES), 0.33 μM (SKES), 0.94 μM (MMH-ES-1), 0.60 μM (STA-ET 7.2), 1.46 μM (A4573), 4.95 μM (PC3), 22.82 μM ( MCF7), 0.82 μM (MDA-MB-231), 1.514 μM (PANC1), 14.28 μM (ASPC1)
体外研究(In Vitro)
YK-4-279 (3-30 μM; overight) dissociates EWS-FLI1 from RHA in Ewing’s sarcoma family tumor (ESFT) cells.
YK-4-279 (3-30 μM; 14 h) nearly eliminates cyclin D1 in TC32 cells.
YK-4-279 (3-30 μM; 72 h) potently and specifically inhibits ESFTs.
YK-4-279 (50 μM; 6 h) induces substantial apoptosis of ESFT cells.
YK-4-279 (0.1-30 μM; 72 h) inhibits the growth of ESFT, prostate, breast and pancreatic cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
YK-4-279 (1.5 mg; i.p. once) inhibited ESFT tumor growth. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Beige mice with orthotopic ESFT and ESFT xenografts
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 25 mg/mL (68.27 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[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.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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