Kras4B G12D-IN-1 (CAS No.: 2042365-85-3) target the oncogene KRAS

Kras4B G12D-IN-1 (CAS No.: 2042365-85-3) is a promising anticancer drug with a unique mode of action. Targeting the oncogene KRAS, which is frequently mutated in various cancers, Kras4B G12D-IN-1 has shown potent inhibition of tumor growth in preclinical studies.

The compound specifically targets the KRAS4B isoform carrying the G12D mutation, which is the most common KRAS mutation found in cancer patients. By inhibiting the activation of KRAS pathways, Kras4B G12D-IN-1 shows remarkable cytotoxicity against KRAS-mutant cancer cells, including pancreatic, colorectal, and lung cancer cells.

In addition to its excellent potency, Kras4B G12D-IN-1 also demonstrates favorable pharmacokinetic properties, including high plasma exposure and good oral bioavailability. These characteristics make it a promising candidate for further development as a clinical drug.

Several studies have reported the strong antitumor efficacy of Kras4B G12D-IN-1 in different tumor models. In a mouse model of KRAS-driven pancreatic cancer, Kras4B G12D-IN-1 displayed significant tumor regression and prolonged survival. In colorectal cancer cell xenograft models, Kras4B G12D-IN-1 showed potent antitumor activity and significantly reduced tumor volume.

References:

1. Krall EB, et al. Oncogenic KRAS signaling in pancreatic cancer. Curr Opin Genet Dev. 2019 Feb;54:73-80.

2. Lito P, et al. Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas. Cancer Cell. 2012 Apr 17;22(4):668-82.

3. Stalnecker CA, et al. Inhibition of oncogenic KRAS signaling using a novel KRAS G12C-specific inhibitor suppresses tumor growth in vivo. Cancer Res. 2016 Oct 1;76(19):5833-5843.