Elironrasib
Based on 3 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.42%
- CAS. Nr.: 2641998-63-0
- Formel: C55H78FN9O8
- Molecular Weight:1012.26
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Elironrasib
More
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
Biologische Aktivität
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KRAS(G12C) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2641998-63-0
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Appearance Solid
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Molecular Weight 1012.26
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Formel C55H78FN9O8
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Color White to off-white
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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
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Synonyms
RMC-6291
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell
2026 May 14;189(10):2918-2933.e17. PMID: 42092352 -
Cell
2024 Oct 31;187(22):6379-6392.e17. PMID: 39255801
Elironrasib purchased from MedChemExpress. Usage Cited in: Cell. 2024 Oct 31;187(22):6379-6392.e17. [Abstract]
Immunoblot analysis was performed on HeLa cells transiently overexpressing K-Ras or K-Ras(G12C). HeLa cells were transiently transfected, treated with different concentrations of RMC-6291 (1 μM and 10 μM) for 3 h, and blotted for Ras, M-Ras, R-Ras, and Rheb.
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Nat Cancer
The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]2026 Jan;7(1):116-130. PMID: 41482524
Elironrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2026 Jan;7(1):116-130. [Abstract]
The Bliss sum of synergy scores for the IK-595 combinations with divarasib, sotorasib, adagrasib, and RMC-6291 was calculated from data obtained from 5‑day CTG assays in the Mia‑PACA‑2 cell line using the integrated synergy score algorithm from the online tool ComBenefit. An integrated score > 10 is considered synergistic (results from a single experiment).
Elironrasib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2026 Jan;7(1):116-130. [Abstract]
Annexin V staining in NCI‑H358 cells treated with DMSO, RMC‑6291 (1 nM), IK‑595 (10 nM), or RMC‑6291 + IK‑595 for 120 h. n = 2 samples per condition from a single experiment.
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (98.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (2.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9879 mL | 4.9394 mL | 9.8789 mL | 24.6972 mL |
| 5 mM | 0.1976 mL | 0.9879 mL | 1.9758 mL | 4.9394 mL | |
| 10 mM | 0.0988 mL | 0.4939 mL | 0.9879 mL | 2.4697 mL | |
| 15 mM | 0.0659 mL | 0.3293 mL | 0.6586 mL | 1.6465 mL | |
| 20 mM | 0.0494 mL | 0.2470 mL | 0.4939 mL | 1.2349 mL | |
| 25 mM | 0.0395 mL | 0.1976 mL | 0.3952 mL | 0.9879 mL | |
| 30 mM | 0.0329 mL | 0.1646 mL | 0.3293 mL | 0.8232 mL | |
| 40 mM | 0.0247 mL | 0.1235 mL | 0.2470 mL | 0.6174 mL | |
| 50 mM | 0.0198 mL | 0.0988 mL | 0.1976 mL | 0.4939 mL | |
| 60 mM | 0.0165 mL | 0.0823 mL | 0.1646 mL | 0.4116 mL | |
| 80 mM | 0.0123 mL | 0.0617 mL | 0.1235 mL | 0.3087 mL |
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