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YK-4-279;≥99% (HPLC)

别名:4,7-二氯-3-羟基-3-(2(4-甲氧基苯基)-2-氧代乙基)二氢吲哚-2-酮;4,7-Dichloro-1,3-dihydro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-2H-indol-2-one

CAS:1037184-44-3;分子式:C17H13Cl2NO4;分子量:366.20;MDL:MFCD18382120
制造商品牌: BSZH 科学公司
货号(SKU): S06076
CAS号: 1037184-44-3
MDL号: MFCD18382120
增值税发票 √ 免费送货 √ 订货电话:010-68689484
¥926.00

产品描述

产品可溶于DMSO (~75mg/mL)

Application

一种致癌转录因子EWS-FLI1与RNA解旋酶A(RHA)结合的有效抑制剂。

YK-4-279 inhibits Ewing's sarcoma family tumor (ESFT) cell growth; YK-4-279 induces apoptosis. IC50 value: Target: RNA Helicase A ES-FLI1 is an oncogenic fusion protein found in Ewing’s sarcoma, a family of undifferentiated tumors that occur throughout the body. The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 μM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5-2 μM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.

YK-4-279抑制尤因氏肉瘤家族肿瘤(ESFT)细胞的生长; YK-4-279诱导细胞凋亡。 IC50值:目标:RNA解旋酶ES-FLI1是一种在尤文氏肉瘤中发现的致癌融合蛋白,尤文氏肉瘤是一类未分化的肿瘤,遍布全身。 RNA解旋酶A(RHA)与ES-FLI1的结合可促进其致癌功能。 YK-4-279是ES-FLI1和RHA之间的蛋白质-蛋白质相互作用的抑制剂。 YK-4-279浓度为10μM时,会阻断RHA与ES-FLI1的结合,并诱导Ewing肉瘤细胞株的凋亡,其IC50值为0.5-2μM。 YK-4-279的剂量为1.5毫克/剂,可在用抑制剂治疗两周后减少尤因肉瘤原位异种移植物在小鼠体内的生长。

性质

Iupac Name4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1,3-dihydro-2H-indol-2-one
Inchi Code1S/C17H13Cl2NO4/c1-24-10-4-2-9(3-5-10)13(21)8-17(23)14-11(18)6-7-12(19)15(14)20-16(17)22/h2-7,23H,8H2,1H3,(H,20,22)
Inchi KeyHLXSCTYHLQHQDJ-UHFFFAOYSA-N


安全信息

符号 
GHS07  GHS07
信号词 Warning
危害声明 H302
警示性声明 P301 + P312 + P330
RIDADR NONH for all modes of transport
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16