| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
Tubulin binds to avanbulin (0–4 μM) as colchicine, with an apparent Kd of 244 nM. [1]. Tubulin undergoes proteolysis when avandulin (50 μM; 0, 10, 20, 30, 60 min) is added [1]. Tiny tubulin aggregates are formed when avanbulin (33 nM; 0, 10, 20, 30, 60 min; HeLa-tubGFP cells) collapses the mitotic spindle [1]. Tubulin oligomers do not form when avandulin is present [1]. In 23 tumor cell lines, avandulin inhibits proliferation with a median relative IC50 of 13.8 nM (96 hours) [2]. GBM6 and GBM9 cell migration is inhibited by avanbulin (6 nM and 20 nM) [3]. GBM6-shEB1 and GBM6-sh0 cells, respectively, respond to avanbulin (6 nM and 20 nM) to initiate GBM6 astrocyte development in an EB1-dependent manner [3]. MG132 (10 μM; 2 h) treated hTert-RPE1 eGFP-α-tubulin cells show decreased kinetochore microtubule (KT–MT) occupancy in response to avanbulin (12 nM; 4 h) [4]. Avanbulin (12 nM; 4 h) exhibits intact spindle shape, decreases the average KT distance of cells, and does not exhibit any chromosome alignment problems [4].
|
|---|---|
| Cell Assay |
Cytotoxicity assay [2]
Cell Types: 23 cell lines, including RD, TC-71, SJ-GBM2, NB-1643. Tested Concentrations: 0.1 nM-1.0 μM Incubation Duration: 96 hrs (hours) Experimental Results: Induced cell growth inhibition with a median relative IC50 of 13.8 nM. |
| References |
|
| Molecular Formula |
C20H17N7O2
|
|---|---|
| Molecular Weight |
387.39
|
| Exact Mass |
387.144
|
| CAS # |
798577-91-0
|
| PubChem CID |
11176685
|
| Appearance |
White to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
771.5±70.0 °C at 760 mmHg
|
| Flash Point |
420.4±35.7 °C
|
| Vapour Pressure |
0.0±2.6 mmHg at 25°C
|
| Index of Refraction |
1.731
|
| LogP |
4.25
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
29
|
| Complexity |
615
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LSFOZQQVTWFMNS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H17N7O2/c21-10-3-11-23-19-18(25-29-26-19)20-24-15-4-1-2-5-16(15)27(20)12-17(28)13-6-8-14(22)9-7-13/h1-2,4-9H,3,11-12,22H2,(H,23,26)
|
| Chemical Name |
3-[[4-[1-[2-(4-aminophenyl)-2-oxoethyl]benzimidazol-2-yl]-1,2,5-oxadiazol-3-yl]amino]propanenitrile
|
| Synonyms |
BAL27862 BAL 27862 BAL-27862 Avanbulin
|
| 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 : ~250 mg/mL (~645.34 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.37 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 20.8 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: ≥ 2.08 mg/mL (5.37 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 20.8 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 | 2.5814 mL | 12.9069 mL | 25.8138 mL | |
| 5 mM | 0.5163 mL | 2.5814 mL | 5.1628 mL | |
| 10 mM | 0.2581 mL | 1.2907 mL | 2.5814 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02490800 | COMPLETEDWITH RESULTS | Drug: Lisavanbulin Phase 1 dose escalation portion Drug: Lisavanbulin Phase 2a expansion portion |
Neoplasms | Basilea Pharmaceutica | 2015-05-20 | Phase 1 Phase 2 |
| NCT02895360 | COMPLETEDWITH RESULTS | Drug: BAL101553 Drug: BAL101553 at MTD |
Neoplasms | Basilea Pharmaceutica | 2016-08-24 | Phase 1 Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
