Kobe2602Kobe2602
MedChemExpress (MCE)
HY-15717
454453-49-7
98.15%
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity.
Kobe2602 (2-20 μM
1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells[1]. Kobe2602 has IC50 value of approximately 10 μM for the cellular Ras-Raf-binding inhibition[1]. Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V[1]. Kobe2602 inhibits Ras?GTP but not Ras?GDP[1]. Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells[1].
Kobe2602 (80 mg/kg
p.o.
five consecutive days per week
for 17 days) exhibits antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-RasG12V gene[1].
Ki: 149 μM (Ras-Raf interaction)[1] In Vitro Kobe2602 (2-20 μM
1 hour) exhibits Ras-Raf-binding inhibition in NIH 3T3 cells[1]. Kobe2602 has IC50 value of approximately 10 μM for the cellular Ras-Raf-binding inhibition[1]. Kobe2602 (20 μM) efficiently inhibits the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V[1]. Kobe2602 inhibits Ras?GTP but not Ras?GDP[1]. Kobe2602 (20 μM) inhibits the anchorage-dependent proliferation of H-RasG12V-transformed cells[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Kobe2602 Related Antibodies Cell Proliferation Assay[1] Cell Line: H-rasG12V-transformed NIH 3T3 cells
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[1]. Shima, Fumi, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proceedings of the National Academy of Sciences of the United States of America (2013), 110(20), 8182-8187, S8182/1-S8182/10. [Content Brief]