Compound Detail
CHEMBL1738
DEXRAZOXANE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1738 |
| Name | DEXRAZOXANE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | BMKDZUISNHGIBY-ZETCQYMHSA-N |
| Therapeutic | ✓ Yes |
3
Targets
4
Activities
2
Assay Types
9
PK Parameters
20
Publications
9
Known Names
15
Indications
2
Mechanisms
Molecular Properties
268.3
MW (Da)
-2.71
ALogP
6
HBA
2
HBD
98.8
PSA (Ų)
0.54
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1995 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Iron sequestering agent | SEQUESTERING AGENT | Iron | ✓ | ✓ |
| DNA topoisomerase II inhibitor | INHIBITOR | DNA topoisomerase II | ✓ | ✓ |
Indications
Hepatoblastoma Leukemia Lymphoma, Large B-Cell, Diffuse Precursor Cell Lymphoblastic Leukemia-Lymphoma Ganglioneuroblastoma Leukemia, Myeloid, Acute Multiple Sclerosis Myelodysplastic Syndromes Neuroblastoma Rhabdomyosarcoma Sarcoma Sarcoma, Ewing Heart Defects, Congenital Neoplasms Osteosarcoma
ATC Classification
V03AF02
dexrazoxane
Level 1: VARIOUS
Level 2: ALL OTHER THERAPEUTIC PRODUCTS
Activity Summary
IC50 3 meas. best 4.75
EC50 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| HL-60 CHEMBL383 | IC50 | 4.75 | 4.75 | 18000.0 | 1 |
| DNA topoisomerase 2-alpha CHEMBL1806 | IC50 | 4.4 | 4.4 | 40000.0 | 1 |
| DNA topoisomerase 2-beta CHEMBL3396 | IC50 | 4.3 | 4.3 | 50000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 2711.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 5573.0 | ng.hr.mL-1 | Canis lupus familiaris |
| CL | 3.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 3.1 | mL.min-1.kg-1 | Homo sapiens |
| Fu | 1.0 | - | Homo sapiens |
| MRT | 3.0 | hr | Homo sapiens |
| T1/2 | 2.5 | hr | Homo sapiens |
| T1/2 | 1.8 | hr | Canis lupus familiaris |
| T1/2 | 1.2 | hr | Canis lupus familiaris |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| HL-60 | IC50 | = | 18000.0 | nM | 4.75 | Antiproliferative activity against human HL-60 cells after 72 hrs by XTT assay | 33750129 |
| DNA topoisomerase 2-alpha | IC50 | = | 40000.0 | nM | 4.4 | Inhibition of human TOP2A assessed as reduction in relaxation of supercoiled DNA... | 33750129 |
| DNA topoisomerase 2-beta | IC50 | = | 50000.0 | nM | 4.3 | Inhibition of human TOP2B assessed as reduction in relaxation of supercoiled DNA... | 33750129 |
Literature References
Data from ChEMBL 36 via Core Engine