AMP423
AMP423 is an oxidation inducer and cell cycle regulator. AMP423 induces necrosis, apoptosis, and reactive oxygen species production. AMP423 induces inhibition of protein synthesis, reduction of thiol levels, and S-phase cell accumulation, and exhibits antitumor activity. AMP423 can be used in research related to multiple myeloma and follicular B-cell lymphoma.
For research use only. We do not sell to patients.
- CAS No.: 219501-57-2
- Formula: C14H11N3O
- Molecular Weight:237.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RPMI-8226 | IC50 |
2.5 μM
|
Cytotoxic activity against human 8226/IM10 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human 8226/IM10 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| MCF7 | IC50 |
36 μM
|
Cytotoxic activity against human MCF7 mammary adenocarcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human MCF7 mammary adenocarcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| RPMI-8226 | IC50 |
3.0 μM
|
Cytotoxic activity against human 8226/S myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human 8226/S myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| RPMI-8226 | IC50 |
3.6 μM
|
Cytotoxic activity against human 8226/Dox40 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human 8226/Dox40 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| U-266 | IC50 |
5.0 μM
|
Cytotoxic activity against human U266 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human U266 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| NCI-H929 | IC50 |
4.6 μM
|
Cytotoxic activity against human NIH-H929 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human NIH-H929 myeloma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| SU-DHL-6 | IC50 |
2.7 μM
|
Cytotoxic activity against human SU-DHL-6 follicular B-cell lymphoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human SU-DHL-6 follicular B-cell lymphoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| Granta-519 | IC50 |
6.0 μM
|
Cytotoxic activity against human Granta 519 mantle cell lymphoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human Granta 519 mantle cell lymphoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| OCI-AML-3 | IC50 |
10.5 μM
|
Cytotoxic activity against human OCI-AML3 acute myelogenous leukemia cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human OCI-AML3 acute myelogenous leukemia cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| MV4-11 | IC50 |
6.2 μM
|
Cytotoxic activity against human MV-4-11 acute myelogenous leukemia cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human MV-4-11 acute myelogenous leukemia cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| MIA PaCa-2 | IC50 |
6.3 μM
|
Cytotoxic activity against human MiaPaCa-2 pancreatic carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human MiaPaCa-2 pancreatic carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| PANC-1 | IC50 |
23.3 μM
|
Cytotoxic activity against human Panc-1 pancreatic carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human Panc-1 pancreatic carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| BXPC-3 | IC50 |
33.4 μM
|
Cytotoxic activity against human BxPC-3 pancreatic carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human BxPC-3 pancreatic carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| MDA-MB-231 | IC50 |
12.0 μM
|
Cytotoxic activity against human MDA-MB231 mammary adenocarcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human MDA-MB231 mammary adenocarcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| HCT-116 | IC50 |
6.7 μM
|
Cytotoxic activity against human HCT-116 colorectal carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human HCT-116 colorectal carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| DU-145 | IC50 |
10.0 μM
|
Cytotoxic activity against human DU-145 prostate carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human DU-145 prostate carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
| PC-3 | IC50 |
17.0 μM
|
Cytotoxic activity against human PC3 prostate carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
Cytotoxic activity against human PC3 prostate carcinoma cells assessed via MTT growth inhibition assay with 72 h incubation.
|
2025.09.06.674656.abstract |
In Vitro
AMP423 potently inhibits the growth of various human cancer cell lines in vitro, with its 72-h IC50 values ranging from 2.5 μM to 36 μM, and shows no cross-resistance in Imexon (HY-15385)-resistant or Doxorubicin (HY-15142A)-resistant myeloma cell lines[1].
AMP423 (2.5-36.0 μM; 72 h) potently inhibits the growth of various human cancer cell lines, with 72-h IC50 values ranging from 2.5 to 36.0 μM, and shows no cross-resistance in ixazomib-resistant or doxorubicin-resistant myeloma cell lines[2].
AMP423 (0.1-100 μM; 72 h) induces cytotoxicity in the human myeloma cell line 8226/S, and this effect is abrogated by continuous exposure to 10 mM N-acetyl cysteine (16 h pre-treatment; 72 h co-incubation), whereas pre-treatment alone without continuous N-acetyl cysteine exposure provides no protective effect[2].
AMP423 (1.25-5.0 μM) reduces the intracellular content of reduced sulfhydryl groups by approximately 30% in 8226/S human myeloma cells, and by approximately 60% in Imexon (HY-15385)-resistant 8226/IM10 human myeloma cells[2].
AMP423 induces caspase-3-dependent apoptosis and necrotic cell death in human 8226/S and 8226/IM10 myeloma cell lines, and its effect on mitochondrial membrane potential is similar to that of imexon[1].
AMP423 (72 h) induces cytotoxicity in human 8226/S myeloma cells, an effect that is antagonized by continuous exposure to 10 mM NAC (16 h pretreatment + 72 h co-incubation), whereas removal of NAC prior to AMP423 exposure abrogates this protective effect[1].
AMP423 reduces the thiol content in human 8226/S myeloma cells by 30% and in human 8226/IM10 myeloma cells by 60%[1].
AMP423 induces reactive oxygen species production in human myeloma cells, with levels comparable to those of Imexon (HY-15385) at equitoxic concentrations[1].
AMP423 (2.5-10.0 μM; 48 h) induces cell death in human myeloma cell lines 8226/S and 8226/IM10 via a combination of apoptosis and necrosis[2].
AMP423 (2.5-10.0 μM; 24-48 h) induces the cleavage of caspase 3 in 8226/S and 8226/IM10 human myeloma cells[2].
AMP423 (2.5-10.0 μM; 24-48 h) induces a concentration-dependent increase in caspase 3 activity in 8226/S and 8226/IM10 human myeloma cells[2].
AMP423 (1.25-5.0 μM) induces S-phase cell accumulation and G1-phase cell depletion in 8226/S and 8226/IM10 human myeloma cells[2].
AMP423 (1.25-5.0 μM; 24-48 h) induces reactive oxygen species production in 8226/S and 8226/IM10 human myeloma cells, with levels comparable to those of Imexon (HY-15385) following treatment at equitoxic concentrations of 1.25, 2.5, and 5.0 μM for 24 h and 48 h[2].
AMP423 (1.25-5.0 μM; 24 h) inhibits protein synthesis in 8226/S and 8226/IM10 human myeloma cells in a concentration-dependent manner at concentrations of 1.25, 2.5, and 5.0 μM, while co-treatment with 10 mM N-acetyl cysteine (HY-B0215) abrogates this activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:8226/S
-
Concentration:10 mM NAC (pretreatment)
-
Incubation Time:16 h (NAC pretreatment); 72 h (AMP423 incubation, with either continuous NAC co-incubation or NAC removal prior to AMP423 addition)
-
Result:Strongly protected 8226/S cells from AMP423-induced cytotoxicity when incubated continuously with 10 mM NAC.
Eliminated the protective effect of NAC when NAC was removed immediately before AMP423 exposure.
-
Cell Line:Multiple human cancer cell lines including multiple myeloma (8226/S, 8226/IM10, 8226/Dox40, U266, NIH-H929), lymphoma (SU-DHL-6, Granta 519), leukemia (OCI-AML3, MV-4-11), pancreatic (MiaPaCa-2, Panc-1, BxPC-3), breast (MCF7, MDA-MB231), colorectal (HCT-116), and prostate (DU-145, PC3) cell lines
-
Concentration:2.5-36.0 μM
-
Incubation Time:72 h
-
Result:Exhibited 72-h IC50 values ranging from 2.5 μM (8226/IM10 myeloma cells) to 36.0 μM (MCF7 breast adenocarcinoma cells).
Showed 72-h IC50 values of 3.0 μM (8226/S), 3.6 μM (8226/Dox40), 5.0 μM (U266), 4.6 μM (NIH-H929), 2.7 μM (SU-DHL-6), 6.0 μM (Granta 519), 10.5 μM (OCI-AML3), 6.2 μM (MV-4-11), 6.3 μM (MiaPaCa-2), 23.3 μM (Panc-1), 33.4 μM (BxPC-3), 12.0 μM (MDA-MB231), 6.7 μM (HCT-116), 10.0 μM (DU-145), and 17.0 μM (PC3).
Demonstrated no cross-resistance in imexon-resistant 8226/IM10 or P-glycoprotein-expressing 8226/Dox40 cells.
-
Cell Line:Human 8226/S myeloma cells, 8226/IM10 imexon-resistant myeloma cells
-
Concentration:2.5-10.0 μM
-
Incubation Time:48 h
-
Result:Induced Annexin V and/or propidium iodide positivity in both 8226/S and 8226/IM10 cells at 48 h, indicating cell death via a mixture of apoptosis and necrosis.
-
Cell Line:Human 8226/S myeloma cells, 8226/IM10 imexon-resistant myeloma cells
-
Concentration:2.5-10.0 μM
-
Incubation Time:24 h; 48 h
-
Result:Detected caspase 3 cleavage in both 8226/S and 8226/IM10 cell lines after treatment.
-
Cell Line:Human 8226/S myeloma cells
-
Concentration:0.1-100 μM (AMP423); 10 mM (N-acetyl cysteine)
-
Incubation Time:16 h (N-acetyl cysteine pretreatment); 72 h (AMP423 incubation)
-
Result:Maintained 8226/S cell survival above 80% even at 100 μM AMP423 when combined with continuous 10 mM N-acetyl cysteine exposure.
Reduced 8226/S cell survival to below 10% at 10 μM AMP423 when N-acetyl cysteine was removed before AMP423 exposure, with survival curves nearly identical to AMP423 alone.
Parmacokinetics
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[3] | 150 mg/kg | i.p. | 5.2 μg/mL |
In Vivo
AMP423 (150 mg/kg; i.p.; Days 1, 5 and 9) achieves a median tumor growth delay of 5 days and a median tumor growth inhibition rate of 82% in SCID mice bearing SU-DHL-6 follicular B-cell lymphoma xenografts[1].
AMP423 (150 mg/kg; i.p.; Days 1, 5 and 9) induces a median tumor growth delay of 21 days and reduces the median tumor volume to 33.3% of that in the control group in SCID mice bearing 8226/S multiple myeloma xenografts[2].
AMP423 (150 mg/kg; i.p.; days 1, 5 and 9) exhibits no significant antitumor activity in SCID mice bearing Imexon (HY-15385)-resistant 8226/IM10 multiple myeloma xenografts, with its median tumor volume reaching 135% of that in the control group and a negative tumor growth delay[2].
AMP423 (150 mg/kg; i.p.; Days 1, 5 and 9) induces a median tumor growth delay of 5 days and reduces the median tumor volume to 82% of that in the control group in SCID mice bearing SU-DHL-6 follicular B-cell lymphoma xenografts[2].
AMP423 (150 mg/kg; i.p.; two treatment cycles with a 5-day interval between cycles) shows no significant anti-tumor activity in SCID mice bearing Granta 519 mantle cell lymphoma xenografts, with its median tumor volume reaching 114% of that in the control group and only extremely slight tumor growth delay[2].
AMP423 (150 mg/kg; i.p.; on days 1, 5, and 9) exhibits no significant antitumor activity in SCID mice bearing 8226/IM10 Imexon (HY-15385)-resistant multiple myeloma xenografts[1].
AMP423 (150 mg/kg; i.p.; with a 5-day interval between two treatment cycles) shows no significant anti-tumor activity in SCID mice bearing Granta 519 mantle cell lymphoma xenografts[1].
AMP423 (200-250 mg/kg; i.p.; single administration) is well tolerated in 7-week-old male SCID mice when administered at a single i.p. dose of 200 mg/kg, with no obvious myelosuppression or nephrotoxicity; however, a single i.p. dose of 250 mg/kg is lethal and induces acute hepatotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:SCID mice[1]
-
Dosage:150 mg/kg
-
Administration:i.p.; on days 1, 5, and 9
-
Result:Produced a median tumor growth delay (T-C) of 21 days.
Produced a median tumor growth inhibition (T/C) of 33.3% relative to vehicle controls.
-
Animal Model:SCID mice[1]
-
Dosage:150 mg/kg
-
Administration:i.p.; on days 1, 5, and 9
-
Result:Produced a median tumor growth delay (T-C) of 5 days.
Produced a median tumor growth inhibition (T/C) of 82% relative to vehicle controls.
-
Animal Model:SCID mice[1]
-
Dosage:150 mg/kg
-
Administration:i.p.; on days 1, 5, and 9
-
Result:Produced a median tumor growth delay (T-C) of -5 days.
Produced a median tumor growth inhibition (T/C) of 135% relative to vehicle controls.
Showed no significant anti-tumor activity.
-
Animal Model:SCID mice[1]
-
Dosage:150 mg/kg
-
Administration:i.p.; two courses separated by 5 days
-
Result:Produced a median tumor growth delay (T-C) of 1 day.
Produced a median tumor growth inhibition (T/C) of 114% relative to vehicle controls.
Showed no significant anti-tumor activity.
-
Animal Model:SCID mice (male, 7 weeks old)[1]
-
Dosage:200 mg/kg; 250 mg/kg
-
Administration:i.p.; single dose
-
Result:Was well-tolerated at a single 200 mg/kg dose, with negligible effects on red and white blood cell counts, normal serum creatinine levels, and normal blood urea nitrogen levels.
Caused lethality in 10/12 mice at 24 hours at a single 250 mg/kg dose, with elevated liver enzymes indicating acute hepatic toxicity.
-
Animal Model:SCID mice[3]
-
Dosage:150 mg/kg
-
Administration:i.p.; on days 1, 5, and 9
-
Result:Produced a median tumor growth delay of 21 days.
Produced a median tumor growth inhibition (T/C) of 33.3% relative to vehicle-treated controls.\nProduced a median tumor growth delay of -5 days.
Produced a median tumor growth inhibition (T/C) of 135% relative to vehicle-treated controls (no significant anti-tumor activity).
-
Animal Model:SCID mice[3]
-
Dosage:150 mg/kg
-
Administration:i.p.; on days 1, 5, and 9
-
Result:Produced a median tumor growth delay of 5 days.
Produced a median tumor growth inhibition (T/C) of 82% relative to vehicle-treated controls.
-
Animal Model:SCID mice[3]
-
Dosage:150 mg/kg
-
Administration:i.p.; two courses with 5 days between courses
-
Result:Produced a median tumor growth delay of 1 day.
Produced a median tumor growth inhibition (T/C) of 114% relative to vehicle-treated controls (no significant anti-tumor activity).
Chemical Information
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CAS No. 219501-57-2
-
Molecular Weight 237.26
-
Formula C14H11N3O
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SMILES
O=C(NC1=C2C=CC=CC2=CC=C1)N3C(C3)C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)