Kobe0065 是一种新颖的，有效的 Ras-Raf 相互作用抑制剂，能够完全抑制 H-Ras·GTP 与 c-Raf-1 RBD 的结合，Ki 值为 46±13 μM。
| 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. |
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| 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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| 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.
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| 分子式 |
C15H11ClF3N5O4S
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| 分子量 |
449.79
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| CAS号 |
436133-68-5
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 溶解性数据 |
In Vitro:
DMSO : ≥ 42.5 mg/mL (94.49 mM) * "≥" means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百 |
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| 科研文献 |
纯度： 98%
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