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Cat. No. Product Name CAS No. Information



ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 of 20.04 nM measured as percentage of NRAS phosphorylation; shows similar IC50 of 23.96 and 27.94 nM for STK19WTWT STK19D89N respectively; displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 uM; efficiently inhibits phosphorylation of NRAS in a dose- and time-dependent manner, inhibits NRAS activity in a dose-dependent manner but does not affect the levels of H3K9 methylation; effectively inhibits NRAS signaling, including the MEK-ERK and PI3K pathways in SK-MEL-2 and WM2032 cells (with NRASQ61R), but the inhibition was much less effective in A375 or UACC62 cells (with NRASWT), effectively inhibits cell growth and induces apoptosis of SK-MEL-2 and WM2032 melanoma cells.




MRTX1257 (MRTX-1257, MRTX 1257) is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM; demonstrates high selectivity toward the Cys12 of KRAS G12C in NCI-H358 cells, without effect on other free cysteine residues; shows sustained regression at 3,10, 30, and 100 mg/kg dose in MIA PaCa-2 xenografts, shows rapid growth inhibition and durable efficacy even after dosing was stopped, and MRTX1257 is orally acitve.


pan-Ras inhibitor 3144


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.




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.




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.




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.


Deltasonamide 2


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.

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