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

Sotorasib  (Synonyms: AMG-510)

Cat. No.: HY-114277 Purity: 99.94%
COA Handling Instructions

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.

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

Sotorasib Chemical Structure

Sotorasib Chemical Structure

CAS No. : 2296729-00-3

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 111 In-stock
Solution
10 mM * 1 mL in DMSO USD 111 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 160 In-stock
50 mg USD 480 In-stock
100 mg USD 840 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Sotorasib:

Sotorasib Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE Sotorasib

WB

    Sotorasib purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2022.

    Sotorasib (1 μM) strongly downregulates survival protein Survivin in MIA PaCa-2 cells.

    View All Ras Isoform Specific Products:

    View All Isoforms
    K-Ras H-Ras Ras

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors[1][2].

    IC50 & Target[1]

    KRAS(G12C)

     

    In Vitro

    In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines[2].
    ? Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC50≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM)[3].

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

    Sotorasib Related Antibodies

    Cell Viability Assay [3]

    Cell Line: NCI-H358 and MIA PaCa-2 cells
    Concentration: 1-10 μM
    Incubation Time: 72 hours
    Result: Potently impaired cellular viability in both NCI-H358 and MIA PaCa-2 (IC50≈0.006 μM and 0.009 μM respectively).
    In Vivo

    In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer[3].

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

    560.59

    Appearance

    Solid

    Formula

    C30H30F2N6O3
    CAS No.
    SMILES

    O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=C2C=C(F)C(C5=C(O)C=CC=C5F)=N4)=O)CC1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (89.19 mM; Need ultrasonic)

    H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7838 mL 8.9192 mL 17.8383 mL
    5 mM 0.3568 mL 1.7838 mL 3.5677 mL
    10 mM 0.1784 mL 0.8919 mL 1.7838 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  20% HP-β-CD in Saline

      Solubility: 10 mg/mL (17.84 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

    • 4.

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

      Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

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

    Purity: 99.94%

    COA (255 KB) HNMR (304 KB) LCMS (265 KB) Elemental Analysis Report (112 KB)

    Handling Instructions (2659 KB)
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Sotorasib 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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Sotorasib2296729-00-3AMG-510AMG510AMG 510RasNSCLCKRASG12Canti-tumourcovalentregressionmutationGDP-boundphosphorylationInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Sotorasib
    Cat. No.:
    HY-114277
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.