| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
After four hours of exposure to both aerobic and hypoxic settings, a panel of ten human cancer cell lines demonstrated the antiproliferative potency of PR-104A (1-100 uM). The H460 non-small cell lung cancer cells had the lowest IC50 (0.51 μM), whereas the greatest IC50 (0.51 μM) was also observed in these cells. 7.3 μM) in prostate cancer cells PC3 [1]. Aldehyde-keto reductase 1C3 catalyzes the fast in vivo conversion of the phosphate ester PR-104 to the alcohol PR-104A, a nitrogen mustard prodrug that is metabolized in hypoxic cells to hydroxylamine (PR-104H) and amine (PR-104M) DNA cross-linking agents [3]. This process occurs independently of oxygen.
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| ln Vivo |
In mice, the phosphate "prodrug" PR-104 is well tolerated and quickly transforms into the matching prodrug PR-104A. PR-104 (total dose: 3.2 mmol/kg) significantly sensitively affected H460 xenografts [1].
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| Cell Assay |
Cell proliferation experiment [1]
Cell Types: HT29, HCT116, C33A SiHa A549, H460, H1299, PC3, SKOV3, A375 Cell Tested Concentrations: 0, 1, 10, 100 uM Incubation Duration: 4 hrs (hours) under aerobic or hypoxic conditions Experimental Results: The IC50 was the lowest in H460 non-small cell lung cancer cells (0.51 μM) and the highest IC50 in PC3 prostate cells (7.3 μM). |
| Animal Protocol |
Animal/Disease Models: Specific pathogen-free homozygous nude mice with H460 xenografts [1]
Doses: Daily (0.23 mmol/kg/dose; qd ×14) or weekly (1.07 mmol/kg/dose; qw ×3 ) Route of Administration: intraperitoneal Experimental Results: Single-agent activity was particularly significant against H460 tumors refractory to docetaxel, cisplatin, gemcitabine, and cyclophosphamide. Daily (qd ×14) versus weekly (qw ×3) regimens were compared with a chemoresistant H460 xenograft model using the same total dose (3.2 mmol/kg) over 14 days, and both regimens were well tolerated. receptive nature. |
| References |
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| Molecular Formula |
C14H19BRN4O9S
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|---|---|
| Molecular Weight |
499.291061639786
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| Exact Mass |
498.006
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| CAS # |
680199-06-8
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| PubChem CID |
9848786
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| Appearance |
Light yellow to green yellow solid powder
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| LogP |
2.92
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
29
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| Complexity |
676
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AZICEEZSDKZDHX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H19BrN4O9S/c1-29(26,27)28-7-5-17(4-2-15)13-11(14(21)16-3-6-20)8-10(18(22)23)9-12(13)19(24)25/h8-9,20H,2-7H2,1H3,(H,16,21)
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| Chemical Name |
2-[N-(2-bromoethyl)-2-(2-hydroxyethylcarbamoyl)-4,6-dinitroanilino]ethyl methanesulfonate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~500.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (12.52 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 62.5 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: ≥ 6.25 mg/mL (12.52 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 62.5 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. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (12.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0028 mL | 10.0142 mL | 20.0284 mL | |
| 5 mM | 0.4006 mL | 2.0028 mL | 4.0057 mL | |
| 10 mM | 0.2003 mL | 1.0014 mL | 2.0028 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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