Chemical Structure : RMC-7977
CAS No.:
2765082-12-8
RMC-7977
(RMC7977, RM-042)
Catalog No.: PC-22112Not For Human Use, Lab Use Only.
RMC-7977 is a potent, highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with Kd of 116 nM, 94.7 nM and 101 nM respectively, KRAS G12V Kd of 85 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
RMC-7977 is a potent, highly selective inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with Kd of 116 nM, 94.7 nM and 101 nM respectively, KRAS G12V Kd of 85 nM.
RMC-7977 is more than tenfold more potent for KRAS than MRAS and other RAS family small GTPase proteins with high sequence identity to KRAS.
RMC-7977 exhibits similar activity for wild-type and mutant RAS variants in biochemical assays
RMC-7977 inhibits the active state of multiple RAS variants.
RMC-7977 exhibits low nanomolar potency for growth inhibition of Matrigel-embedded human KRASG12X-mutant PDAC patient-derived organoids.
RMC-7977 (50 mg/kg, po, q.o.d) inhibits tumor growth and extends survival in autochthonous models of PDAC.
Physicochemical Properties
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M.Wt
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865.11
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Formula
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C47H60N8O6S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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References
1. Urszula N Wasko, et al. bioRxiv. 2023 Dec 4:2023.12.03.569791.
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