| 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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| S8884 |
Adagrasib (MRTX849)
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Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
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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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| E1051 |
MRTX1133
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MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds 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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| 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 signaling 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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| 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-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC).
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Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01075-4
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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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| 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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| E1962 |
Zoldonrasib (RMC-9805)
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Zoldonrasib (RMC-9805) is an orally active inhibitor of KRAS G12D that inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation.
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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 tumor 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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| S8156 |
ARS-853
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ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. This compound also induces apoptosis.
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Sci Rep, 2023, 10.1038/s41598-023-46623-w
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Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00216-8
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SLAS Discov, 2022, S2472-5552(22)12517-7
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