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Cat. No. Product Name CAS No. Information
PC-35878

KRAS-G12C inhibitor 13

2158296-45-6 KRAS-G12C inhibitor 13 is a potnt, irreversible, covalent and in vivo-active inhibitor of KRAS-G12C, suppresses ERK phosphorylation with IC50 of 70 nM in H358 cell assays; displays no significant activity against non-G12C cell lines with IC50 of >16 uM; demonstrates KRAS-G12C target engagement in vivo and antitumor efficacy in the MIA PaCa-2 tumor xenograft models.
PC-35765

KRAS4b-PDEδ stablizer C19

KRAS4b-PDEδ stablizer C19 is a small molecule that binds and stablizes the KRAS4b-PDEδ complex, decreases the viability and proliferation of colorectal cancer cells; showed high cytotoxicity in the colorectal cancer cell lines HCT116 and LoVo, with a stronger effect in KRAS-dependent LoVo cells. Importantly, C19 significantly decreased tumor size in a xenograft mouse model and showed lower side effects than 5-FU.
PC-35613

KBFM123

1090346-46-5 KBFM123 (KBFM-123) is a small molecule, allosteric inhibitor of GTP-bound form of H-Ras, weakly inhibits the association of H-RasG12V-GppNHp with c-Raf-1 RBD (Kd=10-100 uM); interacts directly with a hydrophobic pocket located between Switch I and Switch II and allosterically inhibits the effector interaction by inducing conformational changes in Switch I and its flanking region in the β2-strand, which are directly involved in recognition of the effector molecules including c-Raf-1; KBFM123 is a promising scaffold for the development of Ras inhibitors.
PC-35594

KRAS inhibitor C6ME

KRAS inhibitor C6ME is a small-molecule compound that blocks biochemical and cellular functions of KRASG12V in vitro.
PC-35593

KRAS inhibitor Cmpd2

KRAS inhibitor Cmpd2 is a small-molecule compound that blocks biochemical and cellular functions of KRASG12V with IC50 of 0.8 uM in vitro; inhibits cell proliferation in SW1990 cells with EC50 of 2.7 uM; the potency of Cmpd2 was strongly enhanced when prenylated K-RAS4B is associated with a lipid bilayer.
PC-35587

RAS inhibitor Abd-7

RAS inhibitor Abd-7 is a potent RAS-binding compound (Kd=51 nM) that interacts with RAS in cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signalling; impairs the protein-protein interaction (PPI) of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRASQ61H and HRASG12V, inhibits phosphorylation of both downstream biomarkers in colorectal cancer (DLD-1, KRASG13D) and NSCLC (H538, KRASG12C) human cell lines, with reduction of AKT phosphorylation starting at 2 uM; shows consistent inhibitory effects in the cell-based BRET assay and the biomarker assay.
PC-35391

SOS1 activator 17

2228955-02-8 SOS1 activator 17 is a small molecule activator of guanine nucleotide exchange factor SOS1 with EC50 of 0.8 uM, modulates RAS signaling in vitro; activates the nucleotide exchange process at submicromolar concentrations in vitro, increases levels of active RAS-GTP in HeLa cells, and elicits signaling changes in the MAPK-ERK pathway, resulting in a decrease in pERK1/2T202/Y204 protein levels.

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