Methoxyamine HCl is a novel, potent and orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. Check for active clinical trials or closed clinical trials using this agent.
Physicochemical Properties
| Molecular Formula | CH6CLNO |
| Molecular Weight | 83.5174 |
| Exact Mass | 83.013 |
| CAS # | 593-56-6 |
| Related CAS # | Methoxyamine-d3 Hydrochloride;110220-55-8 |
| PubChem CID | 521874 |
| Appearance | White to off-white solid powder |
| Density | 1.1 g/mL at 25 °C |
| Boiling Point | 105-110°C |
| Melting Point | 151-154 °C(lit.) |
| Index of Refraction | n20/D 1.4021 |
| LogP | 1.008 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 2 |
| Rotatable Bond Count | 0 |
| Heavy Atom Count | 4 |
| Complexity | 4.8 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | XNXVOSBNFZWHBV-UHFFFAOYSA-N |
| InChi Code | InChI=1S/CH5NO.ClH/c1-3-2;/h2H2,1H3;1H |
| Chemical Name | methoxyamine hydrochloride |
| Synonyms | TRC102, TRC 102, TRC-102 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| References | Ger. Offen. to BASF, (1994), DE 4233333 A1 19940407. |
| Additional Infomation |
O-methylhydroxylamine hydrochloride appears as off-white crystals. (NTP, 1992) Methoxyamine Hydrochloride is the hydrochloride salt form of methoxyamine, an alkoxyamine with potential chemotherapeutic adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic DNA damage sites and thereby inhibits base excision repair (BER) process, which may prevent repair of DNA strand breaks and result in an induction of apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~50 mg/mL (~598.66 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (29.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (29.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (29.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 11.9732 mL | 59.8659 mL | 119.7318 mL | |
| 5 mM | 2.3946 mL | 11.9732 mL | 23.9464 mL | |
| 10 mM | 1.1973 mL | 5.9866 mL | 11.9732 mL |