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RMC-5127

CAT: 0804-HY-173629-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-173629-01Size:1 mg
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Description
RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RASG12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V (ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRASG12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer[1].
UNSPSC
12352005
Target
Apoptosis; Ras
Related Pathways
Apoptosis; GPCR/G Protein; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Purity
99.96
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
C[C@H](OC)C1=[C@@]([C@@]2=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H]4OC[C@@H]4C)=O)[C@@H]5N6CC7(COC7)C6)=O)C8CC3C8)=O)C9=C(C=CC(C%10=CSC5=N%10)=C9)N2CCOC%11CCOCC%11)C=C(N%12CCN(C%13CC%13)CC%12)C=N1
Molecular Formula
C57H75N9O9S
Molecular Weight
1062.33
References & Citations
[1]Chen Z, et al. RMC-5127, a first-in-class, orally bioavailable mutant-selective RASG12V (ON) inhibitor is central nervous system (CNS) -penetrant and demonstrates anti-tumor activity in a preclinical intracranial xenograft model[J]. Cancer Research, 2024, 84 (6_Supplement) : 3340-3340.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
K-Ras