| Size | Price | |
|---|---|---|
| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
SPB does not have a specific biological target itself but serves as a drug-linker conjugate for ADCs. The compound consists of Xanthotoxol, a bioactive molecule with anti-inflammatory properties, linked to an antibody via an ADC linker. This design enables the targeted delivery of Xanthotoxol to specific cells or tissues, enhancing its therapeutic efficacy while reducing systemic side effects.
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|---|---|
| ln Vitro |
The in vitro activity of SPB is assessed by its ability to form stable conjugates with antibodies and its anti-inflammatory activity. The efficiency of conjugation to antibodies is evaluated by SDS-PAGE, mass spectrometry, and HPLC. The anti-inflammatory activity of the Xanthotoxol component is confirmed in cell-based assays measuring the production of inflammatory mediators.
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| ln Vivo |
In vivo studies for SPB are typically conducted as part of complete ADC development, where the antibody-drug conjugate is evaluated rather than the linker conjugate alone. The conjugate's performance in vivo is assessed through pharmacokinetic studies, evaluating its stability in circulation, targeting efficiency, and therapeutic efficacy in models of inflammatory diseases.
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| Enzyme Assay |
For conjugation assays, SPB is dissolved in anhydrous DMSO or DMF and added to a solution of antibody in PBS buffer. The reaction is incubated at room temperature, and the extent of conjugation is monitored by SDS-PAGE or MALDI-TOF mass spectrometry. The stability of the conjugate in plasma is also assessed.
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| Cell Assay |
For cellular studies, target cells are cultured and treated with SPB-containing ADC conjugates at various concentrations. The anti-inflammatory activity is assessed by measuring the production of inflammatory cytokines such as TNF-α or IL-6 by ELISA. Cell binding is evaluated by flow cytometry using fluorescently labeled conjugates.
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| Animal Protocol |
For in vivo efficacy studies, appropriate animal models of inflammatory diseases are used. The SPB-containing ADC is administered via intravenous injection. Disease severity is assessed by measuring clinical scores, inflammatory markers, and histopathological analysis of tissues. Pharmacokinetic studies are conducted to determine compound exposure in plasma and target tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SPB are characterized as part of the complete ADC. The compound has a molecular weight of 385.32 and a purity of 98%. It is typically handled as a solid and stored under recommended conditions to maintain stability. Detailed PK parameters such as half-life, clearance, and volume of distribution depend on the specific antibody used in the conjugate.
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| Toxicity/Toxicokinetics |
The toxicity profile of SPB is not explicitly detailed in the provided sources. As a chemical reagent used in ADC development, standard laboratory safety precautions should be followed when handling it. It is intended for research use only and is not for human therapeutic applications. The compound's safety would be evaluated in the context of the complete ADC rather than the linker conjugate alone.
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| Additional Infomation |
SPB is a drug-linker conjugate for ADCs with a molecular formula of C19H15NO8 and a molecular weight of 385.32. It consists of Xanthotoxol linked via an ADC linker and exhibits potent anti-inflammatory activity. This research compound is for laboratory use only and has not been approved for clinical applications.
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| Molecular Formula |
C19H15NO8
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|---|---|
| Molecular Weight |
385.324305772781
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| Exact Mass |
385.079
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| CAS # |
858128-57-1
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| PubChem CID |
15950836
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
1.2
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
688
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C=CC2C(=C(C3=C(C=2)C=CO3)OCCCC(ON2C(=O)CCC2=O)=O)O1
|
| InChi Key |
ZOMXGWWLJXRQKZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15NO8/c21-13-4-5-14(22)20(13)28-16(24)2-1-8-25-19-17-12(7-9-26-17)10-11-3-6-15(23)27-18(11)19/h3,6-7,9-10H,1-2,4-5,8H2
|
| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 4-(7-oxofuro[3,2-g]chromen-9-yl)oxybutanoate
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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 |
| 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 : 50 mg/mL (129.76 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.49 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 | 2.5952 mL | 12.9762 mL | 25.9525 mL | |
| 5 mM | 0.5190 mL | 2.5952 mL | 5.1905 mL | |
| 10 mM | 0.2595 mL | 1.2976 mL | 2.5952 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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