产品信息
抗原名称
H-Ras-cRaf1 interaction
商品描述
Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
分子量
449.79
纯度
>98%
可溶性
DMSO 89 mg/mL (197.87 mM)
Ethanol 13 mg/mL (28.9 mM)
Ethanol 13 mg/mL (28.9 mM)
外观
Powder
In vitro(体外研究)
Kobe0065-family compounds bind to Ras⋅GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras⋅GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition.
In vivo(体内研究)
Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss.
背景
别名
Kobe 0065; Kobe-0065
分子式
C15H11ClF3N5O4S
CAS号
436133-68-5
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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