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Chemical Structure| 2296729-00-3 Chemical Structure| 2296729-00-3

Structure of Sotorasib
CAS No.: 2296729-00-3

Chemical Structure| 2296729-00-3

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Sotorasib is a KRAS G12C inhibitor with an IC50 value of 5.3 nM for KRAS G12C. Sotorasib has antitumor effects and can be used in research on KRAS mutation-associated cancers.

Synonyms: AMG-510

4.5 *For Research Use Only !

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Product Details of Sotorasib

CAS No. :2296729-00-3
Formula : C30H30F2N6O3
M.W : 560.59
SMILES Code : O=C1N(C2=C(C)C=CN=C2C(C)C)C3=NC(C4=C(O)C=CC=C4F)=C(F)C=C3C(N5[C@@H](C)CN(C(C=C)=O)CC5)=N1
Synonyms :
AMG-510
MDL No. :MFCD32062763
InChI Key :NXQKSXLFSAEQCZ-SFHVURJKSA-N
Pubchem ID :137278711

Safety of Sotorasib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Sotorasib

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MIAPACA2 cells 40 nM 72 h Investigate the effect of Sotorasib on MIAPACA2 cells, results showed that ALDH1A1 knockout enhanced the effect of Sotorasib PMC11465744
H2122 cells 100 nM 72 h Investigate the effect of Sotorasib on H2122 cells, results showed that ALDH1A1 knockout enhanced the effect of Sotorasib PMC11465744
MIA PaCa-2 different dose combinations 72 h All three dose combinations demonstrated synergistic inhibition of MIA PaCa-2 cell proliferation (CI <1). PMC10690049
NCI-H358 different dose combinations 72 h Similar synergistic effects (CI <1) in suppressing cell growth were also observed with the NCI-H358 cells. PMC10690049
MIA PaCa-2 Different dose combinations 72 h Synergistic inhibition of MIA PaCa-2 cell proliferation PMC10690049
NCI-H358 Different dose combinations 72 h Synergistic inhibition of NCI-H358 cell proliferation PMC10690049
MIA-PaCa-2 cells 30 nM 2 days Suppressed the activation of MEK/ERK, leading to cell growth inhibition and increased protein aggregation PMC10720158
H358 cells 30 nM 2 days Suppressed the activation of MEK/ERK, leading to cell growth inhibition and increased protein aggregation PMC10720158
MiaPaCa2 6 nM 72 h To evaluate the synergistic effects of Sotorasib with various drugs and identify potential combination therapies PMC11792994
AsPC-1 35 nM 72 h To evaluate the synergistic effects of MRTX1133 with various drugs and identify potential combination therapies PMC11792994
H358 1 µM 72 h Evaluate the anti-proliferative effect of Sotorasib on KRASG12C mutant lung cancer cells PMC11364849
H23 1 µM 72 h Evaluate the anti-proliferative effect of Sotorasib on KRASG12C mutant lung cancer cells PMC11364849
H1792 1 µM 72 h Evaluate the anti-proliferative effect of Sotorasib on KRASG12C mutant lung cancer cells PMC11364849
H2030 1 µM 72 h Evaluate the anti-proliferative effect of Sotorasib on KRASG12C mutant lung cancer cells PMC11364849
H2122 1 µM 72 h Evaluate the anti-proliferative effect of Sotorasib on KRASG12C mutant lung cancer cells PMC11364849
MIA PaCa-2 5 μM > 2 weeks Establish sotorasib-resistant cells PMC10308767
NCI-H23 5 μM > 2 weeks Establish sotorasib-resistant cells PMC10308767
LU65 5 μM > 2 weeks Establish sotorasib-resistant cells PMC10308767

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice UMUC3 and H358 subcutaneous xenograft models Oral gavage 100 mg/kg Once daily until the end of the experiment To evaluate the antitumor efficacy of Sotorasib and its combination with radiolabeled P1B7 IgG. Results showed that the combination of Sotorasib with radiolabeled P1B7 IgG significantly inhibited tumor growth. PMC11733532
Nude mice MIAPACA2 xenograft model Oral 30 mg/kg Once daily for 2 weeks Investigate the anti-tumor effect of Sotorasib in MIAPACA2 xenograft model, results showed that Sotorasib significantly inhibited tumor growth PMC11465744
ICR-SCID mice PDAC (MIA PaCa-2) cell-derived xenograft model oral 25 mg/kg daily for 3 weeks The combination of KPT9274 and Sotorasib significantly reduced tumor volumes, tumor weights, and tumor sizes. PMC10690049
ICR-SCID mice MIA PaCa-2 cell-derived tumor xenograft model Oral 25 mg/kg Daily administration for 3 weeks Significant reduction in tumor volumes, tumor weights, and tumor sizes PMC10690049
Mice MIA-PaCa-2 xenograft tumor model Oral 30 mg/kg Daily for 6 weeks Initially sensitive to sotorasib but relapsed after 6 weeks, with increased protein aggregation and restored proteostasis in relapsed tumors PMC10720158
Mice Subcutaneous tumor model Oral 30 mg/kg Once daily for 3 weeks Evaluate the in vivo anti-tumor effect of Sotorasib on KRASG12C mutant tumors PMC11364849
NOD/SCID mice Subcutaneous xenograft model Oral 10 mg/kg Once daily for 14 days Evaluate the effect of combined treatment with sotorasib and BRAF inhibitor PMC10308767
Mice NCI-H358-R xenograft model Subcutaneous injection 250 mg/kg 4 days on, 2 days off Evaluate the efficacy of GNE-7883 in combination with sotorasib in overcoming KRAS G12C inhibitor resistance PMC10293011

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05327491 Healthy Participants PHASE1 COMPLETED 2022-07-17 Labcorp Clinical Research Unit... More >> - Daytona Beach, Daytona Beach, Florida, 32117-5116, United States|Miami Research Associates LLC - Main Campus / Late Phase, South Miami, Florida, 33143-5026, United States|Labcorp Clinical Research Unit - Dallas, Dallas, Texas, 75247-4989, United States|Labcorp Clinical Research Unit - Madison, Madison, Wisconsin, 53704-2526, United States Less <<
NCT05048784 Healthy Participants PHASE1 COMPLETED 2022-02-18 Covance Clinical Research Unit... More >>, Daytona Beach, Florida, 32117, United States|Covance Clinical Research Unit, Dallas, Texas, 75247, United States Less <<
NCT06807619 Brain Tumor PHASE1 RECRUITING 2025-01-28 Memorial Sloan Kettering at Ba... More >>sking Ridge (Limited Protocol Activities), Basking Ridge, New Jersey, 07920, United States|Memorial Sloan Kettering Monmouth (Limited Protocol Activities), Middletown, New Jersey, 07748, United States|Memorial Sloan Kettering Commack (Limited Protocol Activities), Commack, New York, 11725, United States|Memorial Sloan Kettering Suffolk- Commack (Limited Protocol Activities), Commack, New York, 11725, United States|Memorial Sloan Kettering West Harrison (Limited Protocol Activities), Harrison, New York, 10604, United States|Memorial Sloan Kettering Cancer Center (All Protocol Activities), New York, New York, 10065, United States|Memorial Sloan Kettering Nassau (Limited Protocol Activities), Uniondale, New York, 11553, United States Less <<
NCT04887064 Hepatic Impairment PHASE1 COMPLETED 2022-03-09 Orange County Research Center,... More >> Tustin, California, 92780, United States|Clinical Pharmacology Of Miami LLC, Miami, Florida, 33014, United States|Orlando Clinical Research Center, Orlando, Florida, 32809, United States|American Research Corporation, San Antonio, Texas, 78215, United States|Pinnacle Clinical Research - San Antonio, San Antonio, Texas, 78229, United States Less <<
NCT04933695 Non-small Cell Lung Cancer PHASE2 ACTIVE_NOT_RECRUITING 2026-01-13 Alabama Oncology, Birmingham, ... More >>Alabama, 35243, United States|Arizona Oncology Associates Professional Corporation, Tucson, Arizona, 85711, United States|City of Hope at Long Beach Elm, Duarte, California, 91010, United States|City of Hope National Medical Center, Duarte, California, 91010, United States|Baptist MD Anderson Cancer Center, Jacksonville, Florida, 32207, United States|Northwest Georgia Oncology Centers PC, Marietta, Georgia, 30060, United States|Indiana University Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States|Baptist Health Lexington, Lexington, Kentucky, 40503, United States|Frederick Memorial Hospital, Frederick, Maryland, 21702, United States|Englewood Hospital and Medical Center, Englewood, New Jersey, 07631, United States|Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, 08901, United States|James J Peters VA Medical Center, Bronx, New York, 10468, United States|Laura and Isaac Perlmutter Cancer Center at New York University Langone, New York, New York, 10016, United States|Northport Veterans Affairs Medical Center, Northport, New York, 11768, United States|State University of New York Upstate Medical University, Syracuse, New York, 13210, United States|Duke University Medical Center, Morris Cancer Clinic, Durham, North Carolina, 27710, United States|Allegheny Health Network Cancer Institute at Allegheny General Hospital, Pittsburgh, Pennsylvania, 15212, United States|University of Pittsburgh Medical Center Cancer Pavillion, Pittsburgh, Pennsylvania, 15232, United States|Medical University of South Carolina, Hollings Cancer Center, Charleston, South Carolina, 29425, United States|Texas Oncology - Medical City Dallas, Dallas, Texas, 75230-2510, United States|Texas Oncology - Plano East, Dallas, Texas, 75230-2510, United States|Texas Oncology-Dallas Presbyterian Hospital, Dallas, Texas, 75231, United States|Texas Oncology - Flower Mound, Dallas, Texas, 75234, United States|Texas Oncology - Baylor, Dallas, Texas, 75246, United States|Texas Oncology-Denton, Denton, Texas, 76201, United States|Oncology Consultants PA, Houston, Texas, 77030, United States|University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States|Texas Oncology- Mckinney, McKinney, Texas, 75071, United States|Texas Oncology - Northeast Texas, Paris, Texas, 75460-5004, United States|Gundersen Health System, La Crosse, Wisconsin, 54601, United States|Universite Catholique de Louvain Cliniques Universitaires Saint Luc, Bruxelles, 1200, Belgium|Universitair Ziekenhuis Antwerpen, Edegem, 2650, Belgium|Jessa Ziekenhuis - Campus Virga Jesse, Hasselt, 3500, Belgium|Centre Hospitalier Universitaire de Liege - Sart Tilman, Liege, 4000, Belgium|Odense Universitetshospital, Odense C, 5000, Denmark|Institut Sainte Catherine, Avignon cedex 9, 84918, France|Centre Hospitalier Universitaire Régional de Lille - H?pital Albert Calmette, Lille Cedex, 59037, France|Centre Hospitalier Universitaire de Limoges - Hopital Dupuytren, Limoges Cedex, 87042, France|Centre Hospitalier Universitaire de Montpellier - Val d Aurelle, Montpellier Cedex 5, 34298, France|Hopital Cochin, Paris, 75014, France|Centre Hospitalier Universitaire de Bordeaux - Hopital Haut Leveque, Pessac Cedex, 33604, France|Centre Hospitalier Universitaire de Rennes - Hopital Pontchaillou, Rennes, 35033, France|Centre Hospitalier de Nantes - H?pital Nord La?nnec, Saint Herblain, 44800, France|H?pital Sainte Musse, Toulon Cedex, 83056, France|Centre Hospitalier Universitaire de Toulouse - Hopital Larrey, Toulouse Cedex 9, 31059, France|Klinikum und Fachbereich Medizin Johann Wolfgang Goethe-Universit?t Frankfurt am Main, Frankfurt am Main, 60590, Germany|Asklepios - Fachkliniken München-Gauting, Gauting, 82130, Germany|Universit?tsklinikum K?ln, Koeln, 50937, Germany|Azienda Socio Sanitaria Territoriale di Monza Ospedale San Gerardo, Monza (MB), 20900, Italy|Azienda Ospedaliera di Rilievo Nazionale Specialistica dei Colli Monaldi, Napoli, 80131, Italy|Azienda Ospedaliera Universitaria San Luigi Gonzaga, Orbassano (TO), 10043, Italy|Istituti Fisioterapici Ospitalieri Regina Elena San Gallicano, Rome, 00144, Italy|Nederlands Kanker Instituut Antoni van Leeuwenhoekziekenhuis, Amsterdam, 1066 CX, Netherlands|Hospital del Mar, Barcelona, Catalu?a, 08003, Spain|Hospital de la Santa Creu i Sant Pau, Barcelona, Catalu?a, 08041, Spain|Hospital Universitari i Politecnic La Fe, Valencia, Comunidad Valenciana, 46026, Spain|Hospital Clinico Universitario de Santiago, Santiago de Compostela, Galicia, 15706, Spain|Hospital Universitario Puerta de Hierro Majadahonda, Majadahonda, Madrid, 28222, Spain|Hospital Universitario La Paz, Madrid, 28046, Spain|Gavle Sjukhus, Gavle, 801 87, Sweden|Sahlgrenska Universitetssjukhuset, Goteborg, 413 45, Sweden|Universitetssjukhuset i Linkoping, Linkoping, 581 85, Sweden|Skanes Universitetssjukhus, Lund, 221 85, Sweden|Norrlands Universitetssjukhus, Umea, 901 85, Sweden|Gazi Universitesi Saglik Arastirma ve Uygulama Merkezi Gazi Hastanesi, Ankara, 06560, Turkey|Trakya Universitesi Saglik Arastirma ve Uygulama Merkezi, Edirne, 22030, Turkey|Koc Universitesi Hastanesi, Istanbul, 34010, Turkey Less <<
NCT06061523 Healthy Participants PHASE1 WITHDRAWN 2024-09-09 -
NCT05398094 Non-small Cell Lung Cancer Sta... More >>ge III|KRAS P.G12C Less << PHASE2 RECRUITING 2028-12-31 ICO Badalona, Hospital Germans... More >> Trias i Pujol, Badalona, Barcelona, 08916, Spain|Hospitalario Universitario A Coru?a, A Coru?a, La Coru?a, 15006, Spain|Hospital Universitario Severo Ochoa, Leganés, Madrid, 28911, Spain|Hospital Universitario Puerta de Hierro, Majadahonda, Madrid, 28222, Spain|Hospital de Son Espases, Palma De Mallorca, Mallorca, 07120, Spain|Hospital General Universitario de Alicante, Alicante, 03010, Spain|Hospital Universitari Quiron Dexeus, Barcelona, 08028, Spain|Hospital Universitari Vall d' Hebron, Barcelona, 08035, Spain|Hospital Parc Taulí, Barcelona, 08208, Spain|Hospital De Basurto, Bilbao, 48013, Spain|ICO Girona, Hospital Josep Trueta, Girona, 17007, Spain|Hospital Clínico San Cecilio De Granada, Granada, 18016, Spain|Complejo Hospitalario De Jaén, Jaén, 23007, Spain|Hospital Universitario Lucus Augusti, Lugo, 27003, Spain|Hospital Clínico San Carlos, Madrid, 28040, Spain|Hospital Universitario Fundación Jiménez Díaz, Madrid, 28040, Spain|Hospital Universitari Son Llatzer, Palma De Mallorca, 07198, Spain|Hospital Universitario Virgen Del Rocio, Sevilla, 41013, Spain|Hospital General Universitario De Valencia, Valencia, 46014, Spain|Hospital Universitario La Fe, Valencia, 46026, Spain Less <<
NCT06582771 Non Small Lung Cancer PHASE2 RECRUITING 2025-08-26 Memorial Sloan Kettering Baski... More >>ng Ridge (Limited Protocol Activities), Basking Ridge, New Jersey, 07920, United States|Memorial Sloan Kettering Monmouth (Limited Protocol Activities), Middletown, New Jersey, 07748, United States|Memorial Sloan Kettering Bergen (Limited Protocol Activities), Montvale, New Jersey, 07645, United States|Memorial Sloan Kettering Suffolk - Commack (Limited Protocol Activities), Commack, New York, 11725, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Memorial Sloan Kettering Nassau, Uniondale, New York, 11553, United States|Memorial Sloan Kettering Westchester, West Harrison, New York, 10604, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.92mL

1.78mL

0.89mL

17.84mL

3.57mL

1.78mL

References

 

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