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Chemical Structure| 1352066-68-2 Chemical Structure| 1352066-68-2

Structure of Navtemadlin
CAS No.: 1352066-68-2

Chemical Structure| 1352066-68-2

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AMG-232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction ((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).

Synonyms: Amg-232; KRT-232; AMG 232

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Product Details of Navtemadlin

CAS No. :1352066-68-2
Formula : C28H35Cl2NO5S
M.W : 568.55
SMILES Code : O=C(O)C[C@]1(C)C(N([C@H](CS(=O)(C(C)C)=O)C(C)C)[C@H](C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC(Cl)=C3)C1)=O
Synonyms :
Amg-232; KRT-232; AMG 232
MDL No. :MFCD28009440

Safety of Navtemadlin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HCT116 p53+/+ 0.5 µM 24 hours Evaluate the effect of Navtemadlin on HCT116 p53+/+ cells under hypoxia, results showed Navtemadlin significantly reduced the S phase cell population. PMC10027891
B16-F10 p53+/+ 2 µM 24 hours Evaluate the effect of Navtemadlin on B16-F10 p53+/+ cells under hypoxia, results showed Navtemadlin significantly reduced the S phase cell population. PMC10027891

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Non-small cell lung cancer patient-derived xenograft models (PDXs) Oral 45 mg/kg Once daily, 5 days/week for 3 weeks To evaluate the anti-tumor activity of KRT-232 alone and in combination with trametinib in KRAS-mutant NSCLC PDX models. Results showed that the tumor regression rate after single agent therapy with KRT-232 was 11%, and it increased to 23% when combined with trametinib. PMC7783771
NSG mice EBV-positive B-cell lymphoma xenograft model Oral 45 mg/kg once daily, 5 days per week for 3 weeks navtemadlin significantly inhibited the growth of EBV-positive B-cell lymphoma and induced tumor regression PMC8945299

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05027867 Small-cell Lung Cancer|Small C... More >>ell Lung Carcinoma|Small Cell Lung Cancer Extensive Stage|Small Cell Lung Cancer Recurrent Less << PHASE2 TERMINATED 2022-08-26 Florida Cancer Specialists - 3... More >>840 Broadway, Fort Myers, Florida, 33901, United States|Florida Cancer Specialists - 560 Jackson St, Suite 220, Saint Petersburg, Florida, 33705, United States|Florida Cancer Specialists, West Palm Beach, Florida, 33401, United States|Northwest Georgia Oncology Centers, Marietta, Georgia, 30060, United States|Hematology Oncology Clinic, Baton Rouge, Louisiana, 70809, United States|University Hospitals Cleveland Medical Center, Cleveland, Ohio, 44106, United States|Mark H Zangmeister Center - 3100 Plaza Properties Boulevard, Columbus, Ohio, 43213, United States|SCRI Tennessee Oncology Chattanooga, Chattanooga, Tennessee, 37404, United States|SCRI Tennessee Oncology Nashville, Nashville, Tennessee, 37205, United States|Flinders Medical Centre, Bedford Park, South Australia, 5042, Australia|Centre Hospitalier de Mulhouse - Hopital Emile Muller, Mulhouse, France/Haut-Rhin, 68000, France|Edog - Ico - Ppds, Angers, Maine-et-Loire, 49933, France|H?pital Louis Pradel, Bron, Rh?ne, 69677, France|Hospices Civils de Lyon, Lyon, Rh?ne, 69495, France|H?pital de La Croix Rousse, Pierre-Bénite, Rh?ne, 69310, France|EDOG - Institut Bergonie - PPDS, Bordeaux, 33000, France|CHU de Grenoble, Grenoble, 38043, France|Hopital Nord AP-HM, Marseille, 13915, France|Klinik für Kardiologie, Angiologie und Pneumologie, Esslingen am Neckar, Baden-Württemberg, 73730, Germany|Lungenfachklinik Immenhausen, Immenhausen, Hessen, 34376, Germany|Evangelische Lungenklinik Berlin, Berlin, 13125, Germany|Bacs Kiskun Megyei Korhaz, Kecskemét, Bács-Kiskun, 6000, Hungary|Chungbuk National University Hospital, Cheongju-si, Chungcheongbuk-do, 28644, Korea, Republic of|CHA Bundang Medical Center, CHA University, Seongnam-si, Gyeonggido, 13520, Korea, Republic of|Clinica Universidad Navarra, Pamplona, Navarra, 31008, Spain|Hospital Universitario 12 de Octubre, Alicante, 28007, Spain|Hospital General Universitario de Alicante, Alicante, 3010, Spain|Hospital Universitario Vall d'Hebrón - PPDS, Barcelona, 0825, Spain|Clinica Universidad Navarra - Madrid, Madrid, 28027, Spain|Hospital Universitario La Paz, Madrid, 28046, Spain|Hospital Regional Universitario de Malaga - Hospital Civil, Málaga, 29011, Spain|Hospital Universitario Virgen Macarena, Sevilla, 41071, Spain|Hospital Universitari i Politecnic La Fe de Valencia, Valencia, 46026, Spain Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.79mL

1.76mL

0.88mL

17.59mL

3.52mL

1.76mL

References

 

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