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QuickView for Amsacrine (compound)
PubChem
| Name: | Amsacrine |
|---|---|
| PubChem Compound ID: | 148673 |
| Description: | Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. |
| Molecular formula: | C21H20ClN3O3S |
| Molecular weight: | 429.921 g/mol |
| Synonyms: |
Methanesulfonamide, N-(4-(9-acridinylamino)-3-methoxyphenyl)-, monohydrochloride (9CI); Methanesulfon-m-anisidide, 4'-(9-acridinylamino)-, monohydrochloride; Methanesulfonyl-m-anisidine, 4'-(9-acridinylamino)-, monohydrochloride; N-(4-(9-Acridinylamino)-3-methoxyphenyl)methanesulfonamidemonohydrochloride; EU-0100154; N-(4-(9-Acridinylamino)-3-methoxyphenyl)-methanesulfonamide monohydrochloride; 54301-15-4; NCI-C03190; m-AMSA hydrochloride; M-Amsacrine.
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DrugBank
Identification
| Name: | Amsacrine |
|---|---|
| Name (isomeric): | DB00276 |
| Drug Type: | small molecule |
| Description: | Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. |
| Synonyms: |
M-AMSA; MAMSA; Acridinyl Anisidide
|
| Brand: | Amsidyl, Amsine, Amsidine, AMSA P-D |
| Category: | Intercalating Agents, Antineoplastic Agents |
| CAS number: | 51264-14-3 |
Pharmacology
| Indication: | For treatment of acute myeloid leukaemia. |
|---|---|
| Pharmacology: |
Amsacrine is an aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but...
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| Mechanism of Action: |
Amsacrine binds to DNA through intercalation and external binding. It has a base specificity for A-T pairs. Rapidly dividing cells are two to four times more sensitive to amsacrine than are resting cells. Amsacrine appears to cleave DNA by inducing double stranded breaks. Amsacrine also targets and inhibits topoisomerase II. Cytotoxicity is greates...
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| Absorption: | Poorly absorbed |
| Protein binding: | 96-98% |
| Biotransformation: | Extensive, primarily hepatic, converted to glutathione conjugate. |
| Half Life: | 8-9 hours |
| Toxicity: | Symptoms of overdose include nausea and vomiting, diarrhea, some cardiotoxicity (rarely). |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
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