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Cat. No. Product Name CAS No. Information
PC-62695

pan-Ras inhibitor 3144

1835283-94-7

pan-Ras inhibitor 3144 (Compound 3144) is a multivalent small-molecule, pan-RAS inhibitor with Kd of 4.7/17/6.6/3.7 uM for KRAS G12D/KRAS wt/HRAS/NRAS respectively; shows weak bindinf for RRAS2 (Kd=24 uM) and no activity for other small GTPases in the RAS superfamily; exhibits lethality in cells partially dependent on expression of RAS proteins; has suitable ADME properties and displays anti-tumor activity in xenograft mouse of pancreatic cancer; orally bioavailable.

PC-62496

ARS-1323

1698024-73-5

ARS1323 is a racemic mixture of ARS-1620/R-atropisomer, ARS-1620 is a potent, specific and covalent KRAS G12C inhibitor with >10-fold improved potency over the initial ARS-853.

PC-62495

ARS-1630

1698055-86-5

ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound.

PC-62494

ARS-1620

1698055-85-4

ARS-1620 is a potent, specific and covalent KRAS G12C inhibitor with an observed rate of 1,100±200 M-1S-1, shows >10-fold improved potency over the initial ARS-853; inhibits RAS signaling with IC50 of 120 nM, exhibits a half maximal G12C target engagement (TE50) at 0.3 uM and near complete engagement at 3.0 uM across a panel of cell lines harboring the mutant allele; achieves rapid and sustained in vivo target occupancy to induce tumor regression, and is a novel generation of KRASG12C-specific inhibitor with promising therapeutic potential.

PC-61152

Deltazinone 1

894554-89-3

Deltazinone 1 (Deltazinone1) is a novel highly selective PDEδ inhibitor that inhibits PDEδ/Ras interaction with Kd of 8±4 nM; displays excellent selectivity against a broad panel of pharmacologically relevant proteins; inhibits the PDEδ-Ras interaction in in-cell measurement with Kd of 58±17 nM, exhibits less unspecific cytotoxicity than Deltarasin in a set of human pancreatic cancer cell lines, including KRas mutation and oncogenic KRas-dependence, decreases Ras-mediated signalling in pancreatic cancer cells.

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.

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