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RMC-7977

CAT: 0804-HY-156498-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-156498-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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
CO[C@H](C1=[C@@](C=C(N2CCN(C3CC3)CC2)C=N1)[C@@](N4CC)=C(C5=C4C=CC6=C5)CC(C)(C)COC([C@@H](N7)CCCN7C([C@@H](NC([C@@H]8[C@@H]9[C@H]8COC9)=O)CC%10=NC6=CS%10)=O)=O)C
Molecular Formula
C47H60N8O6S
Molecular Weight
865.11
References & Citations
[1]Singh M, et al. Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy. Research Square; 2023.|[2]Popescu B, et al. RAS MULTI (ON) inhibitor RMC-7977 targets oncogenic RAS mutations and overcomes RAS/MAPK-mediated resistance to FLT3 inhibitors in AML models[J]. Blood, 2023, 142: 2793.|[3]Wasko UN, et al. Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer. Nature. 2024 May;629 (8013) :927-936.
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

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