2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. MRTX1133

MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.

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CAS 番号 : 2621928-55-8

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 119 在庫あり
Solid
5 mg $90 在庫あり
10 mg $150 在庫あり
25 mg $250 在庫あり
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カスタマーレビュー

Based on 46 publication(s) in Google Scholar

Other Forms of MRTX1133:

MRTX1133 関連抗体

Top Publications Citing Use of Products

顧客検証

RT-PCR
WB

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1022-1031.  [Abstract]

    MRTX1133 (10, 100 nM; 24 h). KPC cells were treated for 24 h and analysed using quantitative PCR with reverse transcription (RT–qPCR)

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1022-1031.  [Abstract]

    MRTX1133 (1, 10, 100 nM; 24 h) was used to treat KPC cells for 24 h, and the cells were analysed using immunoblotting.

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2024 Oct 4;14(10):1964-1989.  [Abstract]

    MRTX1133 (0.5 μM; 24 h)-treated 9805 cells produce conditioned medium (CM) that induces a reduction in Il33 expression in CD1WT fibroblasts.

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2024 Nov 4;84(21):3629-3639.  [Abstract]

    PDAC cell lines grown in low confluent collagen cultures were treated with MRTX1133 (0.5 μmol/L) for 8 hours, and the effect on ERK1/2 phosphorylation was analyzed by Western blotting.

    MRTX1133 purchased from MedChemExpress. Usage Cited in: Immunity. 2023 Nov 14;56(11):2570-2583.e6.  [Abstract]

    Western blot showing phosphorylated and total ERK1/2 in lysates of KRASG12D-mutated A427 cells, treated with anti-KRASG12D-IgA1 or MRTX1133.

    Ras アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    K-Ras H-Ras N-Ras Ras

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations[1][2].

    IC50 & Target[1]

    KRas G12D

    0.2 pM (Kd)

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    > 5000 nM
    Compound: 1; MRTX1133
    Antiproliferative activity against human A549 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    Antiproliferative activity against human A549 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    		[PMID: 37921024]
    AGS IC50
    1.4 nM
    Compound: 1; MRTX1133
    Antiproliferative activity against human AGS cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    Antiproliferative activity against human AGS cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    		[PMID: 37921024]
    AGS IC50
    6 nM
    Compound: 1; MRTX1133
    Cytotoxicity against human AGS cells harboring KRAS G12D mutant assessed as reduction in cell viability measured after 3 days by 2D cell viability assay
    Cytotoxicity against human AGS cells harboring KRAS G12D mutant assessed as reduction in cell viability measured after 3 days by 2D cell viability assay
    		[PMID: 34889605]
    ASPC1 IC50
    7.9 nM
    Compound: 1; MRTX1133
    Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    		[PMID: 37921024]
    MKN-1 IC50
    > 3000 nM
    Compound: 1; MRTX1133
    Cytotoxicity against human MKN-1 cells harboring wild type KRAS assessed as reduction in cell viability measured after 3 days by 2D viability assay
    Cytotoxicity against human MKN-1 cells harboring wild type KRAS assessed as reduction in cell viability measured after 3 days by 2D viability assay
    		[PMID: 34889605]
    NCI-H1299 IC50
    > 5000 nM
    Compound: 1; MRTX1133
    Antiproliferative activity against human NCI-H1299 cells harboring KRAS wild type assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    Antiproliferative activity against human NCI-H1299 cells harboring KRAS wild type assessed as inhibition of cell growth incubated for 5 days by crystal violet staining analysis
    		[PMID: 37921024]
    体外実験

    MRTX1133 inhibits ERK phosphorylation in the AGS cell line with an IC50 ranging 1-10 nM (AsPC-1, Panc 04.03, Panc 02.03, SW1990, GP2D, Suit2, A427, SNU1033, and HPAC cells). In a 2D viability assay, the IC50 of MRTX1133 is 6 nM against AGS cells (KRAS G12D), while demonstrating more than 500-fold selectivity against MKN1, a cell line which is dependent on KRAS for its growth and survival due to the amplification of wild-type KRAS[1].

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

    MRTX1133 関連抗体
    体内実験

    MRTX1133 displays efficacious in a KRAS G12D mutant xenograft mouse tumor model[1].

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

    Animal Model: 6-8-weekold, female, athymic nude-Foxn1nu mice (Panc 04.03 model)[1]
    Dosage: 3, 10, or 30 mg/kg
    Administration: Intraperitoneal; twice a day for 28 days
    Result: Resulted in a dose-dependent antitumor activity with 94% growth inhibition observed at 3 mg/kg BID (IP) and tumor regressions of -62% and -73% observed at 10 and 30 mg/kg BID (IP), respectively.
    分子量

    600.63

    分子式

    C33H31F3N6O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OC1=CC(C2=C(F)C3=NC(OC[C@]45C[C@@H](F)CN4CCC5)=NC(N6C[C@H]7N[C@H](CC7)C6)=C3C=N2)=C8C(C#C)=C(F)C=CC8=C1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (83.25 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 1.6649 mL 8.3246 mL 16.6492 mL
    5 mM 0.3330 mL 1.6649 mL 3.3298 mL
    10 mM 0.1665 mL 0.8325 mL 1.6649 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
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: 3.5 mg/mL (5.83 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 3.5 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 (35.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.16 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (16.65 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% SBE-β-CD/50 mM Citrate pH 5.0

      Solubility: 10 mg/mL (16.65 mM); Clear solution; Need ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C

    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.
    純度とドキュメンテーション

    純度: 99.97%

    COA (255 KB) HNMR (148 KB) RP-HPLC (163 KB) LCMS (234 KB)

    取扱説明書 (2659 KB)
    参考文献

    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 1.6649 mL 8.3246 mL 16.6492 mL 41.6230 mL
    5 mM 0.3330 mL 1.6649 mL 3.3298 mL 8.3246 mL
    10 mM 0.1665 mL 0.8325 mL 1.6649 mL 4.1623 mL
    15 mM 0.1110 mL 0.5550 mL 1.1099 mL 2.7749 mL
    20 mM 0.0832 mL 0.4162 mL 0.8325 mL 2.0811 mL
    25 mM 0.0666 mL 0.3330 mL 0.6660 mL 1.6649 mL
    30 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3874 mL
    40 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0406 mL
    50 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8325 mL
    60 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
    80 mM 0.0208 mL 0.1041 mL 0.2081 mL 0.5203 mL
    • No file chosen (Maximum size is: 1024 Kb)
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    MRTX1133 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    MRTX11332621928-55-8MRTX 1133MRTX-1133Rasfirst-in-classactiveinactivestatesmutantwild-typetumorcellsKRASG12DERKphosphorylationInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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