Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
ln Vitro |
In order to actively administer docetaxel (DTX) for the treatment of prostate cancer that expresses the PSMA, DUPA is employed as the targeting moiety[1]. In 22RV1 cell cultures, the DUPA-indenoisoquinoline compound has an IC50 in the low nanomolar range[2].
|
---|---|
ln Vivo |
Tumor growth is completely stopped by the DUPA-indenoisoquinoline conjugate, causing no toxicity, as shown by the treated mice's loss of body weight and death[2].
|
References |
[1]. Peng ZH, et al. Spacer length impacts the efficacy of targeted docetaxel conjugates in prostate-specific membrane antigen expressing prostate cancer. J Drug Target. 2013 Dec;21(10):968-80.
[2]. Roy J, et al. DUPA conjugation of a cytotoxic indenoisoquinoline topoisomerase I inhibitor for selective prostate cancer cell targeting. J Med Chem. 2015 Apr 9;58(7):3094-103. |
Molecular Formula |
C11H16N2O9
|
---|---|
Molecular Weight |
320.253
|
Exact Mass |
320.09
|
Elemental Analysis |
C, 41.26; H, 5.04; N, 8.75; O, 44.96
|
CAS # |
302941-52-2
|
Appearance |
Solid powder
|
SMILES |
O=C(N[C@](CCC(O)=O)([H])C(O)=O)N[C@](CCC(O)=O)([H])C(O)=O
|
Synonyms |
DUPA; FN11; FN-11; FN 11; SWN41522; SWN-41522; SWN 41522;
|
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 |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ≥ 300 mg/mL (~936.77 mM)
H2O : ≥ 150 mg/mL (~468.38 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (23.42 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 75.0 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: ≥ 7.5 mg/mL (23.42 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 75.0 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. View More
Solubility in Formulation 3: ≥ 7.5 mg/mL (23.42 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 | 3.1226 mL | 15.6128 mL | 31.2256 mL | |
5 mM | 0.6245 mL | 3.1226 mL | 6.2451 mL | |
10 mM | 0.3123 mL | 1.5613 mL | 3.1226 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.