| E1858 |
RMC-7977
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RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumour efficacy in pancreatic ductal adenocarcinoma (PDAC).
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Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01075-4
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| E1597 |
Daraxonrasib (RMC-6236)
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Daraxonrasib (RMC-6236) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS.
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Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01075-4
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bioRxiv, 2025, 2025.07.07.663486
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| E1051 |
MRTX1133
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MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly bind to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.
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J Exp Clin Cancer Res, 2025, 44(1):164
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Cell Rep, 2025, 44(6):115774
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Br J Cancer, 2025, 10.1038/s41416-025-03162-7
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| E1962 |
Zoldonrasib (RMC-9805)
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Zoldonrasib (RMC-9805) is an orally active inhibitor of KRAS G12D that inhibits RAS signalling, leading to Apoptosis in cancer cells with the KRAS G12D mutation.
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| S8830 |
AMG 510 (Sotorasib)
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Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
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Cell Res, 2025, 10.1038/s41422-025-01085-9
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Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0450
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Cell Death Dis, 2025, 16(1):661
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| S8959 |
BI-2852
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BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. This compound blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signalling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
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Eur J Cell Biol, 2023, 102(2):151314
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| S8884 |
Adagrasib (MRTX849)
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Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favourable drug-like properties. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signalling.
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Br J Cancer, 2025, 10.1038/s41416-025-03162-7
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iScience, 2025, 28(9):113374
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Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0022
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| E4651 |
HRS-4642
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HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo.
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J Exp Clin Cancer Res, 2025, 44(1):68
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| S8707 |
ARS-1620
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ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C and could achieve rapid and sustained in vivo target occupancy to induce tumour regression.
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iScience, 2025, 28(6):112748
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J Biol Chem, 2025, S0021-9258(25)02386-5
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Res Sq, 2025, rs.3.rs-6264377
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| S8916 |
BI-3406
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BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. This compound reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signalling. It exhibits anti-tumour activities.
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Cell Rep Med, 2025, 6(8):102284
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Cancer Res, 2025, 10.1158/0008-5472.CAN-24-3819
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iScience, 2025, 28(2):111662
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