k-ras(g12d)

KRASG12D-IN-3-D3 is the deuterium labeled KRASG12D-IN-3. KRASG12D-IN-3 (T206049) (compound Z1084) is a KRASG12D inhibitor with oral bioactivity that can effectively inhibit the growth of tumor cells AGS and AsPC-1, with IC50 values of 0.38 nM and 1.23 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.

KRASG12D-IN-6 is a PROTAC target protein ligand used in the synthesis of CH091138. CH091138 is a potent and selective KRASG12D PROTAC degrader with anti-tumor activity.

KRASG12D-IN-7 is a selective inhibitor of KRASG12D. It exhibits strong binding affinity to KRASG12D in both GDP-bound and GTP-bound states, with Kd values of 1.12 nM and 1.86 nM, respectively. This compound inhibits the proliferation of KRASG12D-bearing AsPC-1 cells with an IC50 of 10 nM and disrupts MAPK signaling. In AsPC-1 cells, KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis (apoptosis), and significantly suppresses colony formation. The inhibitor is applicable for research on cancers with KRASG12D mutations, particularly pancreatic ductal adenocarcinoma (PDAC).

Zoldonrasib (RMC-9805) is a mutant-selective covalent KRAS G12D inhibitor with oral activity and significant antitumor activity, inducing tumor cell apoptosis in preclinical models of various KRAS-mutant cancers.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

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

Kras4B G12D-IN-1 is an anticancer agent that functions as an inhibitor of the Kras4B G12D protein. It effectively reduces the expression of Kras protein in mouse embryonic fibroblasts (MEFs) harboring the Kras4B G12D mutation[1].

BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM. BC-LI-0186 competitively binds the RagD interaction site of LRS with Kd of 42.1 nM and has no effect on LRS-vps34, LRS-eprs, RagB-RagD association, mTORC1 complex formation. BC-LI-0186 potently inhibits the activity of tumor-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 can be used for lung cancer-related research.

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 G12D inhibitor 26 (Compound 64B) is an inhibitor of KRAS G12D with an IC50 ≤ 100 nM.

KRAS G12D inhibitor 28 (Compound 1) is an inhibitor of KRAS G12D and can be utilized in cancer research.

PROTACKRAS G12D degrader 2 is a peptidomimetic molecule capable of inducing the degradation of SARS-CoV-2 3-chymotrypsin-like protease (3CLPro). Designed as a PROTAC molecule, it combines a dipeptidyl 3CLPro ligand based on GC-376 with a pomalidomide moiety, linked through a piperazine-piperidine linker.

PROTACKRAS G12D degrader 1 is a potent, rapid, and selective degrader of PROTACKRASG12D, with a DC50 of 38.06 nM. It demonstrates significant antitumor efficacy.

KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor with antitumor activity.

KRAS G12D inhibitor 22 (compound 6) is a KRAS mutation inhibitor with high antitumor activity (IC50 < 100 nM), excellent selectivity, and low toxicity. It is applicable in breast cancer research.

KRAS G12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRAS G12D, with an IC50 of 0.007 μM. It plays a significant role in cancer research.

KRAS G12D inhibitor 29 (Compound Formula (I)) is an orally active and selective inhibitor of KRASG12D. It effectively blocks KRASG12D-mediated downstream signaling pathways, thereby inhibiting the proliferation of tumor cells. This compound holds potential for research into cancers associated with KRASG12D mutations, such as pancreatic cancer, lung cancer, and colorectal cancer.

(R)-KRAS G12D inhibitor 28 hydrochloride dihydrate is the dihydrate hydrochloride salt form of (R)-KRAS G12D inhibitor 28. KRAS G12D inhibitor 28 (Compound 1) acts as an inhibitor of the KRAS G12D protein and is utilized in cancer research.

KRAS G12D-IN-30 (Compound 4) is a KRAS inhibitor. It functions by blocking the activity of the KRAS G12 mutant, thereby inhibiting the activation of downstream MAPK signaling cascade regulators (Raf1-MEK-ERK). KRAS G12D-IN-30 is applicable for cancer research.

KRAS G12D-IN-34 (Compound 13) is a KRAS (G12D) inhibitor with IC50 values of 1.05 nM for KRAS (G12D) and 1.59 μM for KRAS (WT). It is applicable in the study of non-small cell lung cancer.

KRAS G12D-IN-33 (Compound 1) is an inhibitor of KRAS G12D and is applicable in cancer research.