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Kobe0065 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. Kobe0065 reduced the amount of c-Raf-1 associated with H-Ras G12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras. Kobe0065 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras G12V, although the effect was slightly weaker than that of 2 μM sorafenib.
| Molecular Weight | 449.79 |
| Formula | C15H11ClF3N5O4S |
| CAS Number | 436133-68-5 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ras Products |
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| AMG410
AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. |
| HRS-4642
HRS-4642 is a selective KRAS(G12D) inhibitor, with Kd value of 0.083 nM. HRS-4642 has anti-cancer activity. HRS-4642 exhibits significant in vivo potency. |
| AZD0022
AZD0022 is a selective and orally active KRASG12D inhibitor. |
| HH0043
HH0043 is an orally active and potent SOS1 inhibitor, with IC50 value of 5.8 nM. |
| BI-2493
BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. |
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