| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
BV-02 targets the 14-3-3 scaffold protein docking site. It inhibits 14-3-3 protein-protein interactions. By disrupting the interaction between 14-3-3 and its client proteins (such as c-Abl), BV-02 promotes the release of c-Abl and its relocalization to the nucleus and mitochondria, inducing apoptosis. This mechanism is particularly relevant in cells expressing the T315I mutation, which is resistant to imatinib.
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| ln Vitro |
In vitro, BV-02 is a potent inhibitor of 14-3-3 protein-protein interactions. It displays cell toxicity/cytotoxicity against hematopoietic cells expressing imatinib-sensitive wild-type Bcr-Abl and the imatinib-resistant T315I mutation. It promotes apoptotic death in cells expressing wt Bcr-Abl or the T315I mutation. The compound's activity is mediated through the release of c-Abl from 14-3-3.
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| ln Vivo |
In vivo, BV-02 is expected to show efficacy in animal models of chronic myeloid leukemia, including those resistant to imatinib. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for BV-02 involve studying its effect on 14-3-3 protein-protein interactions. Techniques such as fluorescence polarization (FP) or surface plasmon resonance (SPR) can be used to measure the binding of 14-3-3 to its client proteins in the presence and absence of the compound. Cellular assays are used to confirm the functional effects.
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| Cell Assay |
In vitro cellular assays for BV-02 are performed using hematopoietic cells expressing wild-type Bcr-Abl or the T315I mutation. Cells are treated with various concentrations of the compound. Cell viability and apoptosis are assessed using MTT, CellTiter-Glo, or Annexin V/PI staining assays. The relocalization of c-Abl to the nucleus and mitochondria can be confirmed by immunofluorescence or subcellular fractionation.
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| Animal Protocol |
In vivo animal studies with BV-02 would typically be conducted in mouse models of chronic myeloid leukemia, including those with imatinib-resistant T315I mutations. The compound would be administered, and its effects on tumor growth and survival would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of BV-02 are not extensively reported. It has a molecular weight of 377.35 and is soluble in DMSO. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of BV-02 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
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| References |
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| Additional Infomation |
BV-02 is a potent inhibitor of 14-3-3 protein-protein interactions. It promotes apoptosis in cells expressing wild-type Bcr-Abl or the imatinib-resistant T315I mutation. The compound is used in research on chronic myeloid leukemia and is available for research purposes only.
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| Molecular Formula |
C20H15N3O5
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|---|---|
| Molecular Weight |
377.35
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| Exact Mass |
377.101
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| CAS # |
292870-53-2
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| PubChem CID |
1087337
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
593.8±60.0 °C at 760 mmHg
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| Flash Point |
312.9±32.9 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.707
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| LogP |
0.59
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
770
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZFYSDSINNOLWGO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15N3O5/c1-11-16(19(26)23(21(11)2)13-6-4-3-5-7-13)22-17(24)14-9-8-12(20(27)28)10-15(14)18(22)25/h3-10H,1-2H3,(H,27,28)
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| Chemical Name |
2-(1,5-dimethyl-3-oxo-2-phenylpyrazol-4-yl)-1,3-dioxoisoindole-5-carboxylic acid
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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 : ~12.5 mg/mL (~33.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.31 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 12.5 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: ≥ 1.25 mg/mL (3.31 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 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6501 mL | 13.2503 mL | 26.5006 mL | |
| 5 mM | 0.5300 mL | 2.6501 mL | 5.3001 mL | |
| 10 mM | 0.2650 mL | 1.3250 mL | 2.6501 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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