RMC-7977 (RMC7977) | Ras inhibitor | Probechem Biochemicals

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 (RMC7977) 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.

Packing	Price	Stock
5 mg	$128	In stock
10 mg	$198	In stock
25 mg	$348	In stock
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Biological Activity

RMC-7977 (RMC7977) 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

M.Wt	865.11
Formula	C47H60N8O6S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1R,5S)-N-[(7S,13S)-20-[5-(4-cyclopropylpiperazin-1-yl)-2-[(1S)-1-methoxyethyl]-3-pyridinyl]-21-ethyl-17,17-dimethyl-8,14-dioxo-15-oxa-4-thia-9,21,27,28-tetrazapentacyclo[17.5.2.12,5.19,13.022,26]octacosa-1(25),2,5(28),19,22(26),23-hexaen-7-yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide

References

1. Urszula N Wasko, et al. bioRxiv. 2023 Dec 4:2023.12.03.569791.

RMC-7977 (RMC7977, RM-042)

Biological Activity

Physicochemical Properties

References

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