| Stereochemistry | ACHIRAL |
| Molecular Formula | CH5NO |
| Molecular Weight | 47.0565 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CON
InChI
InChIKey=GMPKIPWJBDOURN-UHFFFAOYSA-N
InChI=1S/CH5NO/c1-3-2/h2H2,1H3
| Molecular Formula | CH5NO |
| Molecular Weight | 47.0565 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Methoxyamine (TRC102) is an orally bioavailable small molecule with potential adjuvant activity, that may potentiate the antitumor activity of alkylating agents. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER) that causes topoisomerase II-dependent irreversible strand breaks and apoptosis. Methoxyamine is currently being studied in multiple Phase 1 and Phase 2 clinical trials sponsored by the National Cancer Institute or Case Comprehensive Cancer Center.
Originator
Approval Year
Cmax
AUC
T1/2
Doses
AEs
Sourcing
PubMed
Patents
Sample Use Guides
Twenty-eight patients were treated with TRC102 at 15, 30, 60 or 100 mg/m2/d. The MTD was exceeded at 100 mg/m2/d due to grade
3 anemia in 50 % of patients.
Route of Administration:
Oral
The human colorectal cancer cell line, HT29 were used for activity evaluation. HT29 cells were cultured at a density of 2×104 per well in multiwell plates (24 wells/plate, SPL). After 24 hours, we treated the cells with different concentrations of 5-FU (5-Fluorouracil) (0, 1, 5, 10, 50, 100 µM) or Mx (Methoxyamine) (0, 1, 6, 30, 60, 120 mM). After 24 hours, cell viability was determined by the trypan blue dye exclusion assay.
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SALT/SOLVATE -> PARENT |
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