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Chemical Structure : ERAS-5024
Catalog No.: PC-21263Not For Human Use, Lab Use Only.
ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.
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ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.
ERAS-5024 displays >100-fold cellular selectivity against WT KRAS.
ERAS-5024 demonstrates potent in vitro anti-proliferative activities in a panel of cell lines harboring G12D mutation (AsPC-1, IC50=3.5 nM).
ERAS-5024 is 3-fold more potent than MRTX1133 in the in vitro three-dimensional Cell-Titer Glo (3D CTG) assay with the AsPC-1 cell line, demonstrates more potent in vivo activity than MRTX1133.
ERAS-5024 at 3 and 10 mg/kg inhibited tumor growth by 51% and 77%, respectively, in the KRAS G12D mutant pancreatic ductal adenocarcinoma (PDAC) xenograft model AsPC-1.
| M.Wt | 672.69 | |
| Formula | C33H30F6N6OS | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Cheng H, et al. ACS Med Chem Lett. 2023 Sep 18;14(10):1351-1357.
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