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Chemical Structure : pan-KRAS degrader 4
CAS No.: 2938169-99-2
Catalog No.: PC-23305Not For Human Use, Lab Use Only.
pan-KRAS degrader 4 is a potent, selective, reversible heterobifunctional pan-KRAS PROTAC degrader with Dmax50 of 17 nM in GP5d cells, efficiently degrades 13 of the 17 most prevalent KRAS mutant alleles and KRASWT with single-digit nanomolar potency.
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pan-KRAS degrader 4 is a potent, selective, reversible heterobifunctional pan-KRAS PROTAC degrader with Dmax50 of 17 nM in GP5d cells, efficiently degrades 13 of the 17 most prevalent KRAS mutant alleles and KRASWT with single-digit nanomolar potency.
pan-KRAS degrader 4 exhibits potent cellular VHL-dependent degradation for endogenous KRASG12D (GP5d, DC50=1 nM, Dmax=99.5%) and KRASG12V (SW620, DC50=13 nM, Dmax=89%).
pan-KRAS degrader 4 less potently degrades KRASG12R (DC50=45 nM, Dmax=59%) and KRAS Q61L/K/R (DC50 > 470 nM, Dmax < 60%) in cell lines expressing KRASG12S, KRASG12A, KRASG13D, and KRASQ61H.
pan-KRAS degrader 4 impacts MAPK signaling and cancer cell proliferation, suppresses pERK and DUSP6, inhibits sotorasib-sensitive KRASG12C-mutant cell lines.
pan-KRAS degrader 4 exhibits in vivo DC50 of 851 nM for the GP2d model in NMRI mice (versus 3.6 nM in 10% FCS).
| M.Wt | 989.23 | |
| Formula | C50H60N12O6S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-Pyrrolidinecarboxamide, 1-[(2R)-2-[3-[4-[(3S)-4-[4-[5-[(4S)-2-amino-3-cyano-4,5,6,7-tetrahydro-4-methylbenzo[b]thien-4-yl]-1,2,4-oxadiazol-3-yl]-2-pyrimidinyl]hexahydro-3-methyl-1H-1,4-diazepin-1-yl]butoxy]-5-isoxazolyl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (2S,4R)- |
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1. Popow J, et al. Science. 2024 Sep 20;385(6715):1338-1347.
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