Navtemadlin
Based on 26 publication(s) in Google Scholar
Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.17%
- CAS No.: 1352066-68-2
- 화학식: C28H35Cl2NO5S
- 분자량:568.55
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보관:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Navtemadlin
More- Nat Genet. 2025 Jan;57(1):140-153. [Abstract]
- Cancer Res. 2026 Mar 20:OF1-OF18. [Abstract]
- Sci Transl Med. 2025 Feb 19;17(786):eadn6274. [Abstract]
- Cell Death Discov. 2025 Mar 4;11(1):86. [Abstract]
- Cell Death Discov. 2020 Jul 6;6:57. [Abstract]
- Clin Transl Med. 2022 Jul;12(7):e961. [Abstract]
- Br J Cancer. 2023 May;128(10):1941-1954. [Abstract]
- Cells. 2026 Mar 5;15(5):473. [Abstract]
- BMC Biol. 2017 Nov 9;15(1):108. [Abstract]
- Med Oncol. 2025 Mar 13;42(4):107. [Abstract]
- JCO Precis Oncol. 2024 Sep:8:e2400241. [Abstract]
- iScience. 2024 May 6;27(6):109862. [Abstract]
- Biomedicines. 2022 Mar 10;10(3):638. [Abstract]
- J Cell Sci. 2023 Jan 15;136(2):jcs260270. [Abstract]
- Exp Dermatol. 2022 Aug;31(8):1243-1252. [Abstract]
- Biomed Chromatogr. 2022 Jul 27;e5467. [Abstract]
- Rep Biochem Mol Biol. 2022 Apr;11(1):111-124. [Abstract]
- bioRxiv. 2026 Mar 30.
- bioRxiv. 2026 Jan 20:2026.01.20.700390. [Abstract]
- University of Wisconsin. 2025.
- medRxiv. 2024 Aug 14:2024.08.12.24311893. [Abstract]
- University of Gothenburg. 2023 Jun 27.
- bioRxiv. 2023 Mar 10.
- Patent. US20210379039A1.
- bioRxiv. 2021 Dec.
- Evid Based Complement Alternat Med. 2021 Jul 8:2021:5517143. [Abstract]
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
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IHC
Biological Activity
IC50: 0.6 nM (p53-MDM2 interaction)[1]
Kd: 0.045 nM (MDM2)[1]
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Cell Line
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Type | Value | Description | References |
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| A-375 | IC50 |
0.6 μM
Compound: AMG-232
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Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by WST assay
Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by WST assay
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[PMID: 37130471] |
| CWR22R | IC50 |
0.3 μM
Compound: AMG-232
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Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 37130471] |
| HCT-116 | GI50 |
33 μM
Compound: AMG 232
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Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
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[PMID: 29691156] |
| HCT-116 | GI50 |
7 μM
Compound: AMG 232
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Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis
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[PMID: 29691156] |
| HCT-116 | IC50 |
>25 μM
Compound: 2, AMG 232
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Antiproliferative activity against p53 -deficient human HCT116 cells after 16 hrs by BrdU proliferation assay
Antiproliferative activity against p53 -deficient human HCT116 cells after 16 hrs by BrdU proliferation assay
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[PMID: 24456472] |
| HCT-116 | IC50 |
10 nM
Compound: 2, AMG 232
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Antiproliferative activity against human HCT116 cells expressing p53 wild type after 16 hrs by BrdU proliferation assay
Antiproliferative activity against human HCT116 cells expressing p53 wild type after 16 hrs by BrdU proliferation assay
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[PMID: 24456472] |
| Hepatocyte | IC50 |
6.3 nM
Compound: 1, AMG 232
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Intrinsic clearance in human hepatocytes measured per million cells
Intrinsic clearance in human hepatocytes measured per million cells
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[PMID: 25384157] |
| MDA-MB-231 | IC50 |
>10 μM
Compound: AMG-232
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 37130471] |
| SJSA-1 | ED50 |
2.8 nM
Compound: 2, AMG 232
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Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as unbound concentration causing inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treat
Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as unbound concentration causing inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treat
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[PMID: 24456472] |
| SJSA-1 | ED50 |
9.1 mg/kg
Compound: 2, AMG 232
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Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treated control
Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treated control
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[PMID: 24456472] |
| SJSA-1 | ED50 |
9.1 mg/kg
Compound: 13
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Antitumor activity against human SJSA1 cells xenografted in athymic nude mouse administered once via oral gavage
Antitumor activity against human SJSA1 cells xenografted in athymic nude mouse administered once via oral gavage
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[PMID: 30253242] |
| SJSA-1 | IC50 |
25 nM
Compound: 39; AMG232
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Antiproliferative activity against human SJSA-1 cells
Antiproliferative activity against human SJSA-1 cells
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[PMID: 33423841] |
| SJSA-1 | IC50 |
47 nM
Compound: 1, AMG 232
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Binding affinity to MDM2 in human SJSA1 cells assessed as induction of p21 gene level after 7 hrs by qRT-PCR assay in presence of 10% human serum
Binding affinity to MDM2 in human SJSA1 cells assessed as induction of p21 gene level after 7 hrs by qRT-PCR assay in presence of 10% human serum
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[PMID: 25384157] |
| SJSA-1 | IC50 |
9.1 nM
Compound: 2, AMG 232
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Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum
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[PMID: 24456472] |
| SJSA-1 | IC50 |
9.2 nM
Compound: 1, AMG 232
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Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 16 hrs by Click-iT EdU HCS assay in presence of 10% human serum
Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 16 hrs by Click-iT EdU HCS assay in presence of 10% human serum
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[PMID: 25384157] |
Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines[1].
Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC50=10 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347 and A427 cells.
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Concentration:0-10 μM.
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Incubation Time:72 hours.
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Result:Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN).
Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice[1].
Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo[1].
Navtemadlin causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice (n=10/group) based cancer models[1].
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Dosage:10, 25, 75 mg/kg.
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Administration:Once daily by oral gavage.
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Result:Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED50 of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1352066-68-2
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Appearance Solid
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분자량 568.55
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화학식 C28H35Cl2NO5S
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Color White to light yellow
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SMILES
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
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Synonyms
AMG 232; KRT-232
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (26)
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Journal Impact Factor
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Most Recent
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Nat Genet
2025 Jan;57(1):140-153. PMID: 39774325 -
Cancer Res
Chemoradiation Reprograms Tumor Cells and the Immune Microenvironment in Cervical Cancer. [Abstract]2026 Mar 20:OF1-OF18. PMID: 41860764 -
Sci Transl Med
A window-of-opportunity trial reveals mechanisms of response and resistance to navtemadlin in patients with recurrent glioblastoma. [Abstract]2025 Feb 19;17(786):eadn6274. PMID: 39970230
Navtemadlin purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Feb 19;17(786):eadn6274. [Abstract]
Immunoblotting of BT145 and BT286 cells treated with Navtemadlin (50 nM; 3-48 h) over time.
Navtemadlin purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Feb 19;17(786):eadn6274. [Abstract]
Dose response curves showed the sensitivity of TP53 wild-type GBM cells (BT145 and BT286; yellow), TP53 mutant GBM cells (BT359; red), bone marrow cells (BMMC; gray), human immortalized astrocytes (hAstro; dark gray), and human neural stem cells (hNSC; light gray) to Navtemadlin (1-10000 nM).
Navtemadlin purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Feb 19;17(786):eadn6274. [Abstract]
Immunoblotting of BT145 and BT286 cells treated with increasing concentrations of Navtemadlin (10-1000 nM; 72 h).
Navtemadlin purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Feb 19;17(786):eadn6274. [Abstract]
Effect of increased Navtemadlin (10-1000 nM; 72 h) treatment on death of BT145 and BT286 cells.
Navtemadlin purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Feb 19;17(786):eadn6274. [Abstract]
Navtemadlin (120-240 mg; p.o.; 2 d) significantly increased the percentage of tumor cells expressing CDKN1A and decreased the proliferative marker Ki67 in recurrent TP53 wild-type glioblastoma.
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Cell Death Discov
CeDaD-a novel assay for simultaneous tracking of cell death and division in a single population. [Abstract]2025 Mar 4;11(1):86. PMID: 40038265 -
Cell Death Discov
2020 Jul 6;6:57. PMID: 32655895
Navtemadlin purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2020 Jul 6;6:57. [Abstract]
The effect of AMG-232 on the p53 signaling pathway, and the expression of IL-6 and PD-L1 at different drug doses is assessed by immunoblotting. AMG-232 treatment leads to activation of the p53 signaling pathway in the cancer cells in a dose-dependent manner. The effect of significant reduction in IL-6 expression is observed with AMG-232 in a dose-dependent manner.
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Clin Transl Med
Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology. [Abstract]2022 Jul;12(7):e961. PMID: 35839307 -
Br J Cancer
Functional genomics of human clear cell sarcoma: genomic, transcriptomic and chemical biology landscape for clear cell sarcoma. [Abstract]2023 May;128(10):1941-1954. PMID: 36959380 -
Cells
PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]2026 Mar 5;15(5):473. PMID: 41827906 -
BMC Biol
A yeast two-hybrid system for the screening and characterization of small-molecule inhibitors of protein-protein interactions identifies a novel putative Mdm2-binding site in p53. [Abstract]2017 Nov 9;15(1):108. PMID: 29121928 -
Med Oncol
2025 Mar 13;42(4):107. PMID: 40082344 -
JCO Precis Oncol
Combination of MDM2 and Targeted Kinase Inhibitors Results in Prolonged Tumor Control in Lung Adenocarcinomas With Oncogenic Tyrosine Kinase Drivers and MDM2 Amplification. [Abstract]2024 Sep:8:e2400241. PMID: 39259915 -
iScience
MDM2/MDMX inhibition by Sulanemadlin synergizes with anti-Programmed Death 1 immunotherapy in wild-type p53 tumors. [Abstract]2024 May 6;27(6):109862. PMID: 38784022 -
Biomedicines
High-Throughput Drug Library Screening in Primary KMT2A-Rearranged Infant ALL Cells Favors the Identification of Drug Candidates That Activate P53 Signaling. [Abstract]2022 Mar 10;10(3):638. PMID: 35327440 -
J Cell Sci
2023 Jan 15;136(2):jcs260270. PMID: 36601864 -
Exp Dermatol
Enhanced expression of p21 promotes sensitivity of melanoma cells towards targeted therapies. [Abstract]2022 Aug;31(8):1243-1252. PMID: 35514255 -
Biomed Chromatogr
Quantitation of navtemadlin in human plasma and brain tissue by liquid chromatography-tandem mass spectrometry. [Abstract]2022 Jul 27;e5467. PMID: 35895384 -
Rep Biochem Mol Biol
AMG-232, a New Inhibitor of MDM-2, Enhance Doxorubicin Efficiency in Pre-B Acute Lymphoblastic Leukemia Cells. [Abstract]2022 Apr;11(1):111-124. PMID: 35765530 -
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bioRxiv
TET2 and TP53 Mutations Cooperatively Modulate the Response to Inflammation to Promote Leukemic Transformation. [Abstract]2026 Jan 20:2026.01.20.700390. PMID: 41648254 -
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medRxiv
Surgical window of opportunity trial reveals mechanisms of response and resistance to navtemadlin (KRT-232) in patients with recurrent glioblastoma. [Abstract]2024 Aug 14:2024.08.12.24311893. PMID: 39211865 -
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Evid Based Complement Alternat Med
Berbamine Inhibits Cell Proliferation and Migration and Induces Cell Death of Lung Cancer Cells via Regulating c-Maf, PI3K/Akt, and MDM2-P53 Pathways. [Abstract]2021 Jul 8:2021:5517143. PMID: 34306137
용액&용해도
DMSO : ≥ 50 mg/mL (87.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 1.5 mg/mL (2.64 mM); Clear solution; Need ultrasonic
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.59 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Canon J, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58. [Content Brief]
[2]. Rew Y, et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7589 mL | 8.7943 mL | 17.5886 mL | 43.9715 mL |
| 5 mM | 0.3518 mL | 1.7589 mL | 3.5177 mL | 8.7943 mL | |
| 10 mM | 0.1759 mL | 0.8794 mL | 1.7589 mL | 4.3972 mL | |
| 15 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL | 2.9314 mL | |
| 20 mM | 0.0879 mL | 0.4397 mL | 0.8794 mL | 2.1986 mL | |
| 25 mM | 0.0704 mL | 0.3518 mL | 0.7035 mL | 1.7589 mL | |
| 30 mM | 0.0586 mL | 0.2931 mL | 0.5863 mL | 1.4657 mL | |
| 40 mM | 0.0440 mL | 0.2199 mL | 0.4397 mL | 1.0993 mL | |
| 50 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8794 mL | |
| 60 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7329 mL | |
| 80 mM | 0.0220 mL | 0.1099 mL | 0.2199 mL | 0.5496 mL |
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