2. GPCR/G Protein
  3. Ras
  4. Adagrasib

Adagrasib  (Synonyms: MRTX849)

Cat. No.: HY-130149 Purity: 99.93%
COA Handling Instructions

Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.

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

Adagrasib Chemical Structure

Adagrasib Chemical Structure

CAS No. : 2326521-71-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 127 In-stock
Solid
5 mg USD 74 In-stock
10 mg USD 115 In-stock
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50 mg USD 450 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Adagrasib:

Adagrasib Related Antibodies

Top Publications Citing Use of Products

    Adagrasib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 18.

    Adagrasib (MRTX849; 60 nM-1 µM) induces Fas expression in KrasG12C mutant MIA PaCa-2 cells.

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    K-Ras H-Ras Ras

    • Biological Activity

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    • Customer Review

    Description

    Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction[1][2].

    IC50 & Target

    KRas G12C

     

    In Vitro

    Adagrasib (MRTX849) (0.1-10000 nM; 3-day/2D conditions; 12-day/3D conditions) potently inhibits cell growth in the vast majority of KRAS G12C-mutant cell lines with IC50s ranging between 10 and 973 nM in the 2D format and between 0.2 and 1042 nM in the 3D format[1].
    Adagrasib (0.24-1000 nM; 24 hours) inhibits KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6[1].

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

    Adagrasib Related Antibodies

    Cell Viability Assay[1]

    Cell Line: MIA PaCa-2, H1373, H358, H2122, SW1573, H2030, KYSE-410 cells (G12C); H1299 (WT); A549 (G12S), HCT116 (G13D) cells
    Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
    Incubation Time: 24 hours
    Result: Inhibits cell growth in the vast majority of KRAS G12C-mutant cell lines with IC50 values ranging between 10 and 973 nM in the 2D format and between 0.2 and 1042 nM in the 3D format.

    Western Blot Analysis[1]

    Cell Line: MIA PaCa-2 cells
    Concentration: 0.24, 0.5, 1.0, 2.0, 3.9, 7.8, 15.6, 31.3, 62.5, 125, 250, 500, 1000 nM
    Incubation Time: 24 hours
    Result: Inhibits KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6, each with IC50s in the single-digit nanomolar range in cell lines.
    In Vivo

    Adagrasib (1-100 mg/kg; i.g.; daily until day 16) demonstrates dose-dependent anti-tumor efficacy over a well-tolerated dose range, and the maximally efficacious dose of MRTX849 is between 30-100 mg/kg/day[1].

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

    Animal Model: MIA PaCa-2 model (6-8-week-old, female, athymic nude-Foxn1 nu mice)[1]
    Dosage: 1, 3, 10, 30 and 100 mg/kg
    Administration: Oral gavage; daily until Day 16
    Result: Rapid tumor regression was observed at the earliest posttreatment tumor measurement and animals in the 30 and 100 mg/kg cohorts exhibited evidence of a complete response at study Day 15. Dosing was stopped at study Day 16 and all 4 mice in the 100 mg/kg cohort and 2 out of 7 mice in the 30 mg/kg cohort remained tumor-free through study Day 70.
    Clinical Trial
    Molecular Weight

    604.12

    Appearance

    Solid

    Formula

    C32H35ClFN7O2
    CAS No.
    SMILES

    N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (82.77 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6553 mL 8.2765 mL 16.5530 mL
    5 mM 0.3311 mL 1.6553 mL 3.3106 mL
    10 mM 0.1655 mL 0.8277 mL 1.6553 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.62 mg/mL (4.34 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.93%

    COA (257 KB) HNMR (329 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
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    Adagrasib 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.

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    Keywords:

    Adagrasib2326521-71-3MRTX849MRTX 849MRTX-849RasKRASG12Cselectivecovalentanti-tumorGDP-boundstateinactiveMIA PaCa-2H1373cellsmutantInhibitorinhibitorinhibit

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