gtp-kras

AZD4747 is a selective and potent inhibitor of the mutant GTPase KRASG12C that crosses the blood-brain barrier and has potential antitumor activity for the study of pancreatic and colorectal adenocarcinoma.

RMC-7977 is a highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.

KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells.

KRAS G12D inhibitor 14 is a potent inhibitor of KRAS G12D that binds KRAS G12D protein (Kd: 33 nM). KRAS G12D inhibitor 14 inhibits the active form of KRAS G12D (KRAS G12D-GTP), but not KRAS G13D.

KRAS G12C inhibitor 25 is an inhibitor of KRAS G12C. KRAS G12C inhibitor 25 inhibits the SOS1-assisted GDP/GTP exchange activity of KRAS-G12C mutants with an IC50 value of 0.48 nM.

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells

RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity[1]. RAS/RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1.