Referencia número: HY-119289

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.

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No. CAS: 219501-57-2
Fòrmula: C₁₄H₁₁N₃O
Peso molecular:237.26

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AMP423 Chemical Structure

No. CAS: 219501-57-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
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Actividad biológica

Descripciòn

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 Cytotoxicity Assay^[1]

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 Viability Assay^[2]

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.

Apoptosis Analysis^[2]

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.

Western Blot Analysis^[2]

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 Viability Assay^[2]

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	C_max
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 21 days and a median tumor growth inhibition rate of 33.3% in SCID mice bearing 8226/S multiple myeloma xenografts^[1].
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

No. CAS 219501-57-2
Peso molecular 237.26
Fòrmula C₁₄H₁₁N₃O
SMILES

O=C(NC1=C2C=CC=CC2=CC=C1)N3C(C3)C#N
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Dorr RT, et al. Anti-tumor activity and mechanism of action for a cyanoaziridine-derivative, AMP423. Cancer chemotherapy and pharmacology. 2012 Apr;69(4):1039-49. [Content Brief]

[2]. Hilz E N, et al. Conditioned orienting predicts preference for, and affective response to, amphetamine after multiple exposures in male rats[J]. bioRxiv, 2025: 2025.09. 06.674656.

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AMP423