| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Topoisomerase; Camptothecins
|
|---|---|
| References | |
| Additional Infomation |
The semi-synthetic derivative of camptothecin, CPT-11, exhibits potent antitumor activity against lymphoma, lung cancer, colorectal cancer, gastric cancer, ovarian cancer, and cervical cancer. CPT-11 is a prodrug that is converted into the active metabolite SN-38 in vivo by enzymes such as carboxylesterase. We synthesized a water-soluble non-prodrug camptothecin analog, DX-8951f. DX-8951f showed high in vitro activity against 32 malignant cell lines and significant inhibition of topoisomerase I. The antiproliferative activity of DX-8951f (expressed as average GI50 value) was approximately 6-fold and 28-fold higher than that of SN-38 and SK&F 10486-A (topotecan), respectively. These three camptothecin derivatives exhibited similar differential response patterns in 32 cell lines, meaning their in vitro cytotoxicity profiles were almost identical. Three intravenous injections of DX-8951f at 4-day intervals showed superior antitumor activity against human gastric adenocarcinoma SC-6 xenografts compared to CPT-11 or SK&F 10486-A. Furthermore, it overcame P-glycoprotein-mediated multidrug resistance. These data suggest that DX-8951f possesses high antitumor activity and is a potential therapeutic agent. [2]
|
| Molecular Formula |
C15H17FN2O3
|
|---|---|
| Molecular Weight |
292.3055
|
| Exact Mass |
292.122
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| CAS # |
143655-70-3
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| PubChem CID |
22080992
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| Appearance |
Off-white to gray solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
|
| Heavy Atom Count |
21
|
| Complexity |
454
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC1C([H])=C(C2C(C([H])(C([H])([H])C([H])([H])C=2C=1C([H])([H])[H])N([H])C(C([H])([H])[H])=O)=O)N([H])C(C([H])([H])[H])=O
|
| InChi Key |
UNQLSBJKEGXCGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17FN2O3/c1-7-10-4-5-12(17-8(2)19)15(21)14(10)13(6-11(7)16)18-9(3)20/h6,12H,4-5H2,1-3H3,(H,17,19)(H,18,20)
|
| Chemical Name |
N-(8-acetamido-6-fluoro-5-methyl-1-oxo-3,4-dihydro-2H-naphthalen-2-yl)acetamide
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| Synonyms |
143655-70-3; N,N'-(3-Fluoro-4-methyl-8-oxo-5,6,7,8-tetrahydronaphthalene-1,7-diyl)diacetamide; Exatecan Intermediate 5; N-(8-acetamido-6-fluoro-5-methyl-1-oxo-3,4-dihydro-2H-naphthalen-2-yl)acetamide; MFCD31657913; SCHEMBL20783225; WLZ3834; UNQLSBJKEGXCGH-UHFFFAOYSA-N;
|
| 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 |
| 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: ~25 mg/mL (~85.5 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.2 mg/mL (7.53 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (22.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 2.2 mg/mL (7.53 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 DMSO stock solution (22.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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: ≥ 2.2 mg/mL (7.53 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 DMSO stock solution (22.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4210 mL | 17.1051 mL | 34.2103 mL | |
| 5 mM | 0.6842 mL | 3.4210 mL | 6.8421 mL | |
| 10 mM | 0.3421 mL | 1.7105 mL | 3.4210 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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