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Sotorasib

CHEMBL4535757 Phase 4 ได้รับการอนุมัติ Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
560.6 g/mol
LogP
4.0
Phase
4

Sotorasib is a first-in-class irreversible covalent inhibitor of the KRAS G12C mutant protein, specifically targeting the mutant cysteine-12 residue to lock KRAS in its inactive GDP-bound state, blocking oncogenic RAS signaling in KRAS G12C-mutant non-small cell lung cancer, colorectal cancer, and other solid tumors. By selectively inhibiting the KRAS G12C variant found in approximately 13% of NSCLC patients and other tumors, it suppresses downstream RAS-MAPK and PI3K-AKT signaling driving tumor proliferation. It represents a breakthrough in targeting previously undruggable KRAS oncoproteins.

น้ำหนักโมเลกุล

560.6000 g/mol

LogP

4.00

TPSA

102.00 Ų

Lipinski RO5

ผ่าน

ด้านการรักษา

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Non-Small Cell Lung Cancer Breast Cancer Prostate Cancer Colorectal Cancer

กลไกการออกฤทธิ์

Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream RAS/MAPK signaling.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

กลไก

Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream …

โครงสร้าง 2 มิติ

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
C=CC(=O)N1CCN(c2nc(=O)n(-c3c(C)ccnc3C(C)C)c3nc(-c4c(O)cccc4F)c(F)cc23)[C@@H](C)C1

                

                

                
                

                    
InChI

                    
InChI=1S/C30H30F2N6O3/c1-6-23(40)36-12-13-37(18(5)15-36)28-19-14-21(32)26(24-20(31)8-7-9-22(24)39)34-29(19)38(30(41)35-28)27-17(4)10-11-33-25(27)16(2)3/h6-11,14,16,18,39H,1,12-13,15H2,2-5H3/t18-/m0/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C30H30F2N6O3

                    

                    
                    

                        
HBD / HBA

                        
1 / 7

                    

                    
                    

                        
พันธะที่หมุนได้

                        
5

                    

                    
                    
                    

                        
อะตอมหนัก

                        
41

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
No targets recorded

    
    
Target interaction data is not yet available for this drug.

    



                
            


            
            

                
                


    
    
        
    
    
    
No interactions recorded

    
    
Drug interaction data is not yet available for this compound.

    



                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
คำถามที่พบบ่อย

                

                    
                    

                        
                        

                            
Sotorasib is a first-in-class irreversible covalent inhibitor of the KRAS G12C mutant protein, specifically targeting the mutant cysteine-12 residue to lock KRAS in its inactive GDP-bound state, blocking oncogenic RAS signaling in KRAS G12C-mutant non-small cell lung cancer, colorectal cancer, and other solid tumors. By selectively inhibiting the KRAS G12C variant found in approximately 13% of NSCLC patients and other tumors, it suppresses downstream RAS-MAPK and PI3K-AKT signaling driving tumor proliferation. It represents a breakthrough in targeting previously undruggable KRAS …

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selectively and irreversibly inhibits KRAS G12C, a mutant oncoprotein that drives uncontrolled cell proliferation in a subset of cancers. By locking KRAS in its inactive GDP-bound state, it blocks downstream RAS/MAPK signaling.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Sotorasib is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
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                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL4535757.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 137278711.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
ข้อจำกัดความรับผิดชอบทางการแพทย์

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.