RAS Inhibitor Screening 서비스 | Oncology 분석서비스 | 고마바이오텍

Figure 1. Demonstrative results by NEA-based RAS variant assays. A. KRAS G12D inhibitor MRTX-1133 showed > 100-fold stronger potency than BI-2865, a pan-KRAS inhibitor, in the KRAS G12D assay. B. Similar potencies were obtained between the above-mentioned two RAS inhibitors in the KRAS G12V assay. C. MRTX-1133 showed slightly left-shifted potency compared to BI-2865 in the KRAS G12R assay. AMG-510, a selective KRAS G12C inhibitor, exhibited no inhibition against these three KRAS G12 mutations. N.D.: Not detected.

Table 1. The selectivity and potency of reported KRAS and SOS1 inhibitors were successfully determined. AMG-510 and MRTX-1133 displayed selective and strong inhibition against KRAS G12C and KRAS G12D, respectively. BI-2865 displayed high potent activity across all KRAS variants compared to NRAS and HRAS. BI-3406, a SOS1 inhibitor, showed moderate inhibition against most RAS mutations. ND: Not detected at 100 μM.

Figure 2. OncoPanel RAS mutant cancer cell lines. A. Number of cancer cell lines bearing KRAS (40+), NRAS (18+), and HRAS (7+) mutations. B. Number of cancer cell lines bearing KRAS mutations including G12D (9+), G12V (10+), G12C (4+), and G13D (4+). The cell proliferation assays can be performed in 2D and 3D formats with flexible treatment designs (3-, 5-, 10-day) and multiple readouts (HCA and CTG).

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