Elironrasib

Elironrasib is an orally active and covalent inhibitor of KRASG12C (ON) . Elironrasib forms a tri-complex within tumor cells between KRASG12C (ON) and cyclophilin A (CypA) . Thus, Elironrasib prevents KRASG12C (ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM[1][2].

Product Specifications

CAS Number

[2641998-63-0]

Product Name Alternative

RMC-6291

UNSPSC

12352005

Target

Apoptosis; ERK; Ras

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; MAPK/ERK Pathway; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/rmc-6291.html

Purity

99.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C[C@H](OC)C(N=CC=C1)=[C@@]1[C@](N2CC)=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H](C(C)C)N(C(C4(F)CCN(C(C#CC(N(C)C)(C)C)=O)CC4)=O)C)=O)C[C@H]5CN6CCO5)=O)CCC3)=O)C7=C2C=CC6=C7

Molecular Formula

C55H78FN9O8

Molecular Weight

1012.26

References & Citations

[1]Nichols R J, et al. RMC-6291, a next-generation tri-complex KRASG12C (ON) inhibitor, outperforms KRASG12C (OFF) inhibitors in preclinical models of KRASG12C cancers[J]. Cancer Research, 2022, 82 (12_Supplement) : 3595-3595. |[2]Cristina Blaj, et al. Enhancement of anti-tumor immunity in immunogenic and immune-refractory RAS mutant tumors with tri-complex RAS (ON) inhibitors, revmed, #PB044, 2022|[3]Schulze CJ, et al. Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS. Science. 2023 Aug 18;381 (6659) :794-799.