1. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  2. Ras ERK Apoptosis
  3. 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.

For research use only. We do not sell to patients.

CAS No. : 2641998-63-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
WB
Cell Proliferation/Viability Assay
Flow Cytometry

    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.

    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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

    IC50 & Target[1]

    KRAS(G12C)

     

    In Vivo

    Elironrasib (200mg/kg, p.o., qd for 60 d) significantly inhibits tumor growth and induce immunological memory in murine tumor models[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    1012.26

    Formula

    C55H78FN9O8

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.9879 mL 4.9394 mL 9.8789 mL
    5 mM 0.1976 mL 0.9879 mL 1.9758 mL
    View the 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.

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    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
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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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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.65%

    References

    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
    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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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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