| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| ln Vitro |
Duocarmycin SA (DSA) (0.1-1 nM; 72 hours) decreases U-138 cell pathway survival in a dose-dependent manner and activates insets and endpoints [2]. Duocarmycin SA (0.1-1 nM; 72 hours) flow chart.
|
|---|---|
| ln Vivo |
In CDF1 mice implanted with mouse liver cancer P388, duocarmycin SA (0.143 mg/kg, intraperitoneal injection, single dose) shown anti-tumor efficacy, considerably prolonging carotene in mice by 30% [3]. Mice lacking CDF1 were given a transplant of murine lymphocytic leukemia P388 [3].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: U-138 Cell Tested Concentrations: 0.1, 0.5, 1 nM Incubation Duration: 72 hrs (hours) Experimental Results: Produced a significant concentration-dependent decrease in cell viability, and tumor cells were more sensitive to proton radiation [2]. 65% cell viability was observed at 0.1 nM, cell viability stabilized at at least 25% at 0.5 nM, and no increase in cytotoxicity was observed at higher doses. The IC50 of Duocarmycin SA against U-138 MG cells is 0.4 nM. Exhibits strong cytotoxicity with an IC50 of 0.0018 nM (1.8 pM). Apoptosis analysis [1] Cell Types: U-138 Cell Tested Concentrations: 0.001, 0.1 nM Incubation Duration: 3 or 14 days Experimental Results: Improved radiosensitivity of U-138 GBM cells by activating apoptosis and necrosis pathways. Survival rates were Dramatically diminished at different proton radiation doses (1-8 Gy). |
| Animal Protocol |
Animal/Disease Models: Murine lymphocytic leukemia P388 transplanted in CDF1 mice [3]
Doses: 0.143 mg/kg Route of Administration: intraperitoneal (ip) injection (i.p.), single dose Experimental Results:demonstrated a significant 30% increase in life span. |
| References |
|
| Additional Infomation |
Duocarmycin SA is an indolecarboxamide.
Duocarmycin sa has been reported in Streptomyces with data available. |
| Molecular Formula |
C25H23N3O7
|
|---|---|
| Molecular Weight |
477.46600
|
| Exact Mass |
477.154
|
| CAS # |
130288-24-3
|
| PubChem CID |
115369
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.53±0.1 g/cm3
|
| Vapour Pressure |
8.82E-25mmHg at 25°C
|
| LogP |
2.74
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
35
|
| Complexity |
971
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
COC1=C(C(=C2C(=C1)C=C(N2)C(=O)N3C[C@H]4C[C@@]45C3=CC(=O)C6=C5C=C(N6)C(=O)OC)OC)OC
|
| InChi Key |
VQNATVDKACXKTF-XELLLNAOSA-N
|
| InChi Code |
InChI=1S/C25H23N3O7/c1-32-17-6-11-5-14(26-19(11)22(34-3)21(17)33-2)23(30)28-10-12-9-25(12)13-7-15(24(31)35-4)27-20(13)16(29)8-18(25)28/h5-8,12,26-27H,9-10H2,1-4H3/t12-,25-/m1/s1
|
| Chemical Name |
methyl (1R,12S)-7-oxo-10-(5,6,7-trimethoxy-1H-indole-2-carbonyl)-5,10-diazatetracyclo[7.4.0.01,12.02,6]trideca-2(6),3,8-triene-4-carboxylate
|
| 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 (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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~104.72 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.47 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 50.0 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: ≥ 5 mg/mL (10.47 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 50.0 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 | 2.0944 mL | 10.4719 mL | 20.9437 mL | |
| 5 mM | 0.4189 mL | 2.0944 mL | 4.1887 mL | |
| 10 mM | 0.2094 mL | 1.0472 mL | 2.0944 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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