Lisavanbulin
Based on 1 Customer Validation
Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator. Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.24%
- No. CAS: 1263384-43-5
- Fòrmula: C26H29N9O3
- Peso molecular:515.57
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
Lisavanbulin (0-50 nM) has a cytostatic and cytolytic effect on SB28 cells with an IC50 of 5.5 nM[4].
Lisavanbulin (0-10 nM) increases the extracellular release of high mobility group box (HMGB1) in SB28 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SB28 glioma implanted orthotopic C57BL/6J mice[4]
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Dosage:25 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Resulted in prolonged survival of mice.
Delayed SB28 growth.
Significantly upregulated the expression of B2m, H2.D1, and H2.K1, coding for MHC-I chains.
Increased the levels of IFN-γ-regulated genes.
Increased survival compared with control mice by 81% when combined with aCD40.
Resulted in less infiltration in tumors due to BM-derived macrophages.
Chemical Information
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No. CAS 1263384-43-5
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Appearance Solid
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Peso molecular 515.57
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Fòrmula C26H29N9O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C(CN2C3=CC=CC=C3N=C2C4=NON=C4NCCC#N)=O)C=C1)[C@@H](N)CCCCN
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Synonyms
BAL-101553
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (193.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Joerger, M., et al., (2023). Safety and anti-tumor activity of lisavanbulin administered as 48-hour infusion in patients with ovarian cancer or recurrent glioblastoma: a phase 2a study. Investigational new drugs, 41(2), 267–275. [Content Brief]
[3]. Holdhoff, M., et al., (2024). Lisavanbulin (BAL101553), a novel microtubule inhibitor, plus radiation in patients with newly diagnosed, MGMT promoter unmethylated glioblastoma. Neuro-oncology advances, 6(1), vdae150. [Content Brief]
[4]. Genoud, V., et al., (2021). Treating ICB-resistant glioma with anti-CD40 and mitotic spindle checkpoint controller BAL101553 (lisavanbulin). JCI insight, 6(18), e142980. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9396 mL | 9.6980 mL | 19.3960 mL | 48.4900 mL |
| 5 mM | 0.3879 mL | 1.9396 mL | 3.8792 mL | 9.6980 mL | |
| 10 mM | 0.1940 mL | 0.9698 mL | 1.9396 mL | 4.8490 mL | |
| 15 mM | 0.1293 mL | 0.6465 mL | 1.2931 mL | 3.2327 mL | |
| 20 mM | 0.0970 mL | 0.4849 mL | 0.9698 mL | 2.4245 mL | |
| 25 mM | 0.0776 mL | 0.3879 mL | 0.7758 mL | 1.9396 mL | |
| 30 mM | 0.0647 mL | 0.3233 mL | 0.6465 mL | 1.6163 mL | |
| 40 mM | 0.0485 mL | 0.2425 mL | 0.4849 mL | 1.2123 mL | |
| 50 mM | 0.0388 mL | 0.1940 mL | 0.3879 mL | 0.9698 mL | |
| 60 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2425 mL | 0.6061 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1940 mL | 0.4849 mL |
Lisavanbulin Related Classifications
HY-19916 Related Classifications
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