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Elironrasib

CAT: 0804-HY-153346-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-153346-01Size:1 mg
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
K-Ras

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A24117-5Elironrasib (RMC-6291) 5mg
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A24117-50Elironrasib (RMC-6291) 50mg
A24117-1Elironrasib (RMC-6291) 1mg

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