RMC-5127

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].

Product Specifications

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.