| Size | Price | Stock | Qty |
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| 50mg |
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| Other Sizes |
| Targets |
The primary target of BPTF-IN-BZ1 is BPTF (bromodomain PHD finger transcription factor), a chromatin remodeling complex component involved in gene transcription. The compound binds to BPTF with high affinity (Kd = 6.3 nM) and shows excellent selectivity over BET bromodomains (>350-fold). By inhibiting BPTF, the compound modulates gene expression and can be used to study the role of BPTF in various biological processes.
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| ln Vitro |
In vitro, BPTF-IN-BZ1 demonstrates potent and selective inhibition of BPTF with a Kd of 6.3 nM. The compound shows >350-fold selectivity over BET bromodomains, indicating high target specificity. It is cell-active, meaning it can penetrate cell membranes and inhibit BPTF in cellular models. The compound's binding affinity and selectivity have been characterized in biochemical and cellular assays. The exact IC₅₀ values for cellular activity are not provided in the available literature.
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| ln Vivo |
In vivo activity of BPTF-IN-BZ1 has not been extensively characterized. As a BPTF inhibitor, it has potential for studying the role of BPTF in various disease models, including cancer. However, detailed in vivo efficacy and pharmacokinetic data are limited in the available literature. The compound's cell-active nature suggests it may have in vivo activity, but further studies would be needed to confirm this.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for BPTF-IN-BZ1 typically involve binding affinity studies using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The compound is incubated with recombinant BPTF protein at varying concentrations (0.1-1000 nM), and the dissociation constant (Kd) is calculated. Selectivity against BET bromodomains is assessed by testing the compound against BRD2, BRD3, BRD4, and BRDT. The compound demonstrates high affinity and selectivity for BPTF.
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| Cell Assay |
In vitro cellular assays for BPTF-IN-BZ1 involve testing its effects on BPTF-dependent gene expression and cell function. Cells are treated with varying concentrations of BPTF-IN-BZ1 (0.01-10 µM) for 24-72 hours. BPTF target gene expression is measured by qRT-PCR or RNA-seq. Cell proliferation and viability are assessed using MTT or CCK-8 assays. The compound demonstrates concentration-dependent inhibition of BPTF activity in cellular models.
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| Animal Protocol |
In vivo animal studies for BPTF-IN-BZ1 are limited, as the compound is primarily used in research to study BPTF function. For efficacy testing, tumor-bearing xenograft models could be used to assess the compound's anti-tumor activity. Animals would be treated with BPTF-IN-BZ1 via oral or intraperitoneal administration at various doses. However, detailed in vivo protocols are not well established in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of BPTF-IN-BZ1 include a molecular weight of 278.74 and a molecular formula of C₁₃H₁₅ClN₄O. The compound is intended for research use only and has not been approved for clinical use. Detailed pharmacokinetic parameters such as half-life, oral bioavailability, and tissue distribution are not well characterized in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of BPTF-IN-BZ1 has not been extensively characterized. As a research compound, standard toxicity studies would include assessment of acute oral toxicity, repeated-dose toxicity, and genotoxicity in animal models. The compound is intended for research use only and is not approved for clinical use. Further toxicological studies would be needed to fully establish its safety profile for therapeutic applications.
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| References | |
| Additional Infomation |
BPTF-IN-BZ1 (CAS 2766623-38-3) has a molecular formula of C₁₃H₁₅ClN₄O and a molecular weight of 278.74. It is a potent, selective, cell-active inhibitor of BPTF with a Kd of 6.3 nM and >350-fold selectivity over BET bromodomains. The compound appears as a light yellow to brown solid powder with a purity of ≥98%. It is intended for research use only and is not approved for clinical use. The compound is used to study the role of BPTF in gene transcription and epigenetic regulation.
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| Molecular Formula |
C13H15CLN4O
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|---|---|
| Molecular Weight |
278.74
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| Exact Mass |
278.093
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| CAS # |
2766623-38-3
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| PubChem CID |
162640908
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.34±0.1 g/cm3(Predicted)
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| Boiling Point |
395.1±52.0 °C(Predicted)
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| LogP |
1.4
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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 |
4
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| Heavy Atom Count |
19
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| Complexity |
399
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C(=O)C(=C(C=N1)NC2=CC=C(C=C2)CCN)Cl
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| InChi Key |
UOQAFGWMKNIVAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H15ClN4O/c1-18-13(19)12(14)11(8-16-18)17-10-4-2-9(3-5-10)6-7-15/h2-5,8,17H,6-7,15H2,1H3
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| Chemical Name |
5-[4-(2-aminoethyl)anilino]-4-chloro-2-methylpyridazin-3-one
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 250 mg/mL (896.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.46 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 (7.46 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 20.8 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: ≥ 2.08 mg/mL (7.46 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 | 3.5876 mL | 17.9379 mL | 35.8757 mL | |
| 5 mM | 0.7175 mL | 3.5876 mL | 7.1751 mL | |
| 10 mM | 0.3588 mL | 1.7938 mL | 3.5876 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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