产品
编 号：F357919
分子式：C15H11ClF3N5O4S
分子量：449.79
分子式：C15H11ClF3N5O4S
分子量：449.79
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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50mg
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100mg
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200mg
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结构图
CAS No: 436133-68-5
产品详情
生物活性：
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
体内研究：
Kobe0065 and Kobe2602 exhibit antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras(G12V) gene by oral administration.
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. The phosphorylation of downstream kinases MEK and ERK is effectively attenuated by 20 μM Kobe0065 and Kobe2602 in NIH3T3 cells transiently expressing H-RasG12V.
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
体内研究：
Kobe0065 and Kobe2602 exhibit antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras(G12V) gene by oral administration.
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. The phosphorylation of downstream kinases MEK and ERK is effectively attenuated by 20 μM Kobe0065 and Kobe2602 in NIH3T3 cells transiently expressing H-RasG12V.
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