2. GPCR/G Protein MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Ras PERK
  4. Daraxonrasib

Daraxonrasib  (Synonyms: RMC-6236; RAS-IN-2)

Cat. No.: HY-148439 Purity: 99.96%
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Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors.

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

CAS No. : 2765081-21-6

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

Based on 10 publication(s) in Google Scholar

Daraxonrasib Related Antibodies

Top Publications Citing Use of Products

    Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946.  [Abstract]

    Proliferation assay of treatment with DMSO or Daraxonrasib (5 nM; 3 days) in HOS and 143B cell lines.

    Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946.  [Abstract]

    HOS-143B cells were seeded in 96-well plates, scratched with a 200 µl pipette tip, and then incubated overnight with DMSO or Daraxonrasib (5 nM and 10 nM). Medium containing 0.1% serum was used as a negative control.

    Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946.  [Abstract]

    HOS-143B cells were treated with daraxonrasib (5 nM and 10 nM; 24 h) . Daraxonrasib treatment downregulated ERK1/2 phosphorylation.

    Daraxonrasib purchased from MedChemExpress. Usage Cited in: PLoS One. 2025 Aug 8;20(8):e0329946.  [Abstract]

    Gelatin zymography demonstrated that Daraxonrasib (5 nM and 10 nM; 48 h) inhibited MMP1 activity in HOS-143B cells.

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    K-Ras H-Ras N-Ras Ras

    • Biological Activity

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    • References

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    Description

    Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors[1][2][3].

    IC50 & Target[1]

    KRas G12D

     

    In Vitro

    Daraxonrasib (EC50 of 1.2 nM for HPAC cells and 1.4 nM for Capan-2 cells; 120 h) potently inhibits the growth of KRAS mutant cancer cell lines HPAC and Capan-2[1].
    Daraxonrasib (10 nM; 0-48 h) cannot durably inhibit mTOR activity when used alone in GP2D colorectal cancer cells, but it can control the rebound of mTOR activity when combined with KO-2806[2].

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

    Daraxonrasib Related Antibodies
    In Vivo

    Daraxonrasib (3-25 mg/kg; p.o.; single dose) shows dose-dependent blood and tumor exposure in the Capan-2 xenograft tumor-bearing BALB/c nude mouse model, with tumor exposure approximately 3-7 times higher than that in blood and relatively slower elimination from tumors[1].
    Daraxonrasib (10-25 mg/kg; p.o.; once daily; 4 weeks) shows dose-dependent antitumor activity in a series of human tumor xenograft models harboring prevalent KRAS mutations (such as Capan-2, NCI-H441, HPAC, NCI-H358, etc.)[1].
    Daraxonrasib (25 mg/kg; p.o.; once daily) can arrest tumor growth when used alone in xenograft models of KRASG12C-mutant NCI-H2122 non-small cell lung cancer and KRASG12D-mutant GP2D colorectal cancer, and it can lead to significant tumor regression when combined with KO-2806[2].

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

    811.05

    Formula

    C44H58N8O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@H]1NN(C([C@H](CC2=NC3=CS2)NC([C@H]4C[C@@H]4C)=O)=O)CCC1)OCC(C)(C)CC5=[C@@](N(CC)C6=C5C=C3C=C6)[C@@]7=C([C@H](C)OC)N=CC(N8CCN(C)CC8)=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 (123.30 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 1.2330 mL 6.1648 mL 12.3297 mL
    5 mM 0.2466 mL 1.2330 mL 2.4659 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

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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 (3.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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 (3.08 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.96%

    SDS (393 KB)

    COA (255 KB) HNMR (360 KB) RP-HPLC (258 KB) LCMS (339 KB)

    Handling Instructions (2659 KB)
    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 1.2330 mL 6.1648 mL 12.3297 mL 30.8242 mL
    5 mM 0.2466 mL 1.2330 mL 2.4659 mL 6.1648 mL
    10 mM 0.1233 mL 0.6165 mL 1.2330 mL 3.0824 mL
    15 mM 0.0822 mL 0.4110 mL 0.8220 mL 2.0549 mL
    20 mM 0.0616 mL 0.3082 mL 0.6165 mL 1.5412 mL
    25 mM 0.0493 mL 0.2466 mL 0.4932 mL 1.2330 mL
    30 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0275 mL
    40 mM 0.0308 mL 0.1541 mL 0.3082 mL 0.7706 mL
    50 mM 0.0247 mL 0.1233 mL 0.2466 mL 0.6165 mL
    60 mM 0.0205 mL 0.1027 mL 0.2055 mL 0.5137 mL
    80 mM 0.0154 mL 0.0771 mL 0.1541 mL 0.3853 mL
    100 mM 0.0123 mL 0.0616 mL 0.1233 mL 0.3082 mL
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    Daraxonrasib Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Daraxonrasib2765081-21-6RMC-6236 RAS-IN-2RMC6236RMC 6236RasPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseG12DK-RasCapan-2NCI-H441HPACNCI-H358Inhibitorinhibitorinhibit

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