kras g12c inhibitor 2

KRas G12C inhibitor 2 is a compound specifically designed to inhibit the KRas G12C mutation.

KRAS G12C inhibitor 29 is an inhibitor of KRAS G12C and can be used to study cancer.

KRAS G12C inhibitor 22 is a specific inhibitor of the KRAS G12C mutation.

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 G12C inhibitor 21 is a specific inhibitor targeting the KRAS G12C mutation.

KRAS G12C Inhibitor 28 is a compound that effectively inhibits the KRAS G12C mutation, exhibiting potent antitumor effects with an inhibitory concentration (IC50) of 57 nanomoles (nM).

KRAS G12C inhibitor 20 is an inhibitor specifically targeting the KRAS G12C mutation.

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

K-Ras G12C-IN-2 is a covalent KRAS G12C inhibitor.

MEK/RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK/RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

KRAS G12D inhibitor 25 (Compound 148) acts as an inhibitor for KRAS G12C and HSP90α, displaying IC50 values of <0.1 μM and 0.1-1 μM respectively. Additionally, it suppresses the proliferation of MIA PaCa-2 and NCI-H358 cell lines, with EC50 values of <0.1 μM and 0.1-1 μM correspondingly. This compound also promotes the degradation of ERBB2, exhibiting a DC50 of 0.1-1 μM.

KRAS inhibitor-37 (compound 2) is a potent inhibitor of KRAS, exhibiting low dissociation constants (KD) with various KRAS mutations: wild type (0.004 nM), G12D (0.041 nM), G12C (0.019 nM), and G12V (0.144 nM). This compound effectively inhibits cell proliferation, demonstrating half-maximal inhibitory concentrations (IC50) ranging from <2 nM to 14 nM in H358, SW620, and PANC08.13 cell lines. KRAS inhibitor-37 holds potential for cancer research applications.

KRAS G12C inhibitor 69 (Compound K09) is an inhibitor of the mutant RAS protein KRAS G12C with an IC50 of 4.36 nM. In the cell lines NCI-H358 and MIA-PACA-2, it suppresses ERK phosphorylation with IC50 values of 12 nM and 7 nM, respectively. Additionally, KRAS G12C inhibitor 69 hinders the proliferation of NCI-H358 and MIA-PACA-2 cancer cells, with IC50 values of 3.15 nM and 2.33 nM, respectively.

KRASG12D-IN-5 (Compound 241) is an orally active KRAS(G12D) inhibitor with an IC50 of 11 nM. It demonstrates potent anticancer activity without significant cytotoxicity to BxPC-3 cells (wild-type), KRAS-mutant AsPC-1 cells (G12D), and MIAPaCa-2 cells (G12C), with CC50 values of 10.37, 0.76, and 0.3 μM, respectively. KRASG12D-IN-5 is applicable in cancer studies, including lung, pancreatic, and colorectal cancers.

KRAS G12C-IN-77 is a selective dual-state covalent inhibitor for KRASG12C, capable of binding with high affinity to the GDP-bound (inactive state) [IC50= 7 nM] and GTP-bound (active state) [IC50= 4 nM] forms of KRASG12C. It swiftly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits the proliferation of KRASG12C-mutant cells. KRAS G12C-IN-77 is applicable in research concerning KRASG12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer.

KRAS inhibitor-15 (compound 3-19) is a potent inhibitor of KRAS G12C with an IC50 of 0.954 μM. It exhibits p-ERK inhibition in MIA PaCA-2 and A549 cells with IC50s of 2.03 μM and >33.3 μM, respectively. KRAS inhibitor-15 has potential for study in pancreatic, colorectal, and lung cancers.

KRAS inhibitor-12 (compound 6-1) is a potent inhibitor of KRAS G12C (IC50: 0.537 μM), exhibiting p-ERK inhibition in MIA PaCA-2 and A549 cells with IC50 values of 1.3 and 3.7 μM, respectively. KRAS inhibitor-12 has potential for study in pancreatic, colorectal, and lung cancers.

KRAS inhibitor-16 (compound 3-11) is a potent inhibitor of KRAS G12C (IC50: 0.457 μM) and exhibits p-ERK inhibition in MIA PaCA-2 and A549 cells with IC50s of 3.06 and 11.1 μM, respectively. KRAS inhibitor-16 has potential for study in pancreatic, colorectal, and lung cancers.

KRAS inhibitor-18 (compound 3-10) is a potent inhibitor of KRAS G12C (IC50: 4.74 μM) and exhibited p-ERK inhibition in MIA PaCA-2 and A549 cells with IC50s of 66.4 μM and 11.1 μM, respectively. KRAS inhibitor-18 has potential for pancreatic, colorectal, and lung cancer studies.

KRAS inhibitor-17 (compound 3-9) is a potent inhibitor of KRAS G12C with an IC50 of 3.37 μM. It exhibits p-ERK inhibition with an IC50 of 9.25 μM in MIA PaCA-2 cells and greater than 33.3 μM in A549 cells. KRAS inhibitor-17 has potential applications in the study of pancreatic, colorectal, and lung cancers.

KRAS inhibitor-13 (compound 5-6) is a potent inhibitor of KRAS G12C (IC50: 0.883 μM) and demonstrates a p-ERK inhibitory effect in MIA PaCA-2 and A549 cells with IC50 values of 5.9 μM and >100 μM respectively. KRAS inhibitor-13 has potential applications in pancreatic, colorectal, and lung cancer studies.

KRAS inhibitor-14 is a potent inhibitor of KRAS G12C (IC50: 0.249 μM). KRAS inhibitor-14 exhibited p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 1.12, >33.3 μM, respectively. KRAS inhibitor-14 has potential to be investigated in pancreatic, colorectal and lung cancers.

KRAS G12C inhibitor 47 is a potent inhibitor of KRAS G12C (IC50: 0.172 μM). KRAS G12C inhibitor 47 exhibits p-ERK inhibition in MIA PaCA-2 cells, A549 cells with IC50 values of 0.046 μM and 69.8 μM respectively. KRAS G12C inhibitor 47 showed investigational potential against pancreatic, colorectal and lung cancers.

KRAS G12C inhibitor 44 is a potent, orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 exhibits anti-proliferative effects in MIA PaCA-2 (IC50: 0.016 μM), H358 cells (IC50: 0.028 μM). inhibitor 44 has anti-tumour activity in vivo.