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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-61154

Deltasonamide 2

2088485-34-9

Deltasonamide 2 (Deltasonamide-2) is a novel small molecule inhibitor of PDE6δ/KRas interaction with Kd of 385 pM; inhibits PDE6δ/KRas interaction in cells with Kd of 64 nM, selectively inhibits growth of KRas mutated and -dependent cells, inhibits the oncogenic KRas-dependent MiaPaCa-2 with IC50 of 750 nM.

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-35953

KRAS G12C inhibitor 11

2158297-63-1 KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 5 nM; demonstrates super proportional dose ascending oral exposure in mice with 3h target coverage at the 30 mg/kg dose; shows rapid growth inhibition and durable efficacy even after dosing was stopped, orally active.

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