SOS1-IN-1 是一种选择性的变构 SOS1 抑制剂。 SOS1-IN-1 抑制变构位点活化，并部分抑制催化位点活化。 SOS1-IN-1 具有抗癌作用。
SOS1-IN-1 is a SOS1 inhibitor.
The growth inhibitory rate (IR)=(average OD value in the control group-average OD value in the treatment group)/average OD value in the control group×100% are compared. Treatments with SOS1-IN-1 at 40 μM and NSC-658497 at 30 μM result in growth inhibitory rate of 29% and 8% respectively. The combination treatment results in growth inhibitory rate of 54%, showing the synergistic effect of SOS1-IN-1 and NSC-658497 on cell growth inhibition. It is showed that the treatment with NSC-658497 at 40 μM for 2 hours alone or in combìnation with the treatment with 40 μM of SOS1-IN-1 overnight resulted in lower expression levels of P-AKT and P-ERK. The treatment wlth 40 μM of SOS1-IN-1 overnight resulted in lower expression levels of P-ERK[1].
[1]. ARYL SULFONOHYDRAZIDES. WO 2016077793A1.
Cell experiment: | MIA paca-2 cells (KRAS G12 C) are subjected to a 3-day proliferation assay following treatment with SOS1-IN-1 (NSC-70220: 40 μM), treatment with NSC-658497 (30 μM) and treatment with a combination of SOS1-IN-1 (40 μM) and NSC-658497 (30 μM). DMSO is used as the negative control[1]. |
参考文献: [1]. ARYL SULFONOHYDRAZIDES. WO 2016077793A1. | |
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