RMC-7977
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM) . It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRASG12C cancer models, and demonstrates good tolerability across various RAS cancer models[1][2][3].
Product Specifications
CAS Number
2765082-12-8
UNSPSC
12352005
Target
AMPK; Apoptosis; ERK; PARP; Raf; Ras; Ribosomal S6 Kinase (RSK)
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; Epigenetics; GPCR/G Protein; MAPK/ERK Pathway; PI3K/Akt/mTOR; Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/rmc-7977.html
Concentration
10mM
Purity
99.48
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
Molecular Formula
C47H60N8O6S
Molecular Weight
865.11
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
C-Raf; H-Ras; K-Ras; N-Ras
Available Sizes
Frequently Asked Questions
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