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RMC-9805 (KRAS G12D inhibitor 18) is a potent and orally active KRAS G12D inhibitor. RMC-9805 induces apoptosis in KRAS G12D mutant cancer cells. RMC-9805 has the potential for the research of KRAS G12D mutant cancer[1][2]. | [in vivo]
RMC-9805 (100 mg/kg; po; once daily for 4-8 days) shows antitumor activity in KRAS G12D xenograft models[2].
| Animal Model: | Mice[2] | | Dosage: | 100 mg/kg | | Administration: | PO; once daily for 4-8 days | | Result: | Decreased the level of myeloid cells, such as mMDSC, gMDSC, M2 TAMS, increased the level of cytotoxic T cells including CD3e+, CD4+, CD8+ T cells. |
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KRAS(G12D) | [References]
[1] BLAKE JAMES F, et al. Preparation of peptide-linked macrocyclic dipeptides as Ras inhibitors.World Intellectual Property Organization, WO2023060253 A1 2023-04-13
[2] Knox,?J et al.RMC-9805, a first-in-class, mutant-selective, covalent and orally bioavailable KRASG12D(ON) inhibitor, promotes cancer-associated neoantigen recognition and synergizes with immunotherapy in preclinical models.?Cancer Res?1 April 2023; 83 (7_Supplement): 3475 |
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