| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
BCL6-IN-7 targets the B-cell lymphoma 6 (BCL6) protein, a transcriptional repressor that plays a crucial role in the development and progression of various types of cancer. It is a potent BCL6 protein-protein interaction (PPI) inhibitor. By inhibiting BCL6, it disrupts the transcriptional repression of target genes involved in cell cycle regulation and apoptosis.
|
|---|---|
| ln Vitro |
In vitro, BCL6-IN-7 inhibits BCL6 protein-protein interactions. By disrupting BCL6-mediated transcriptional repression, it may reactivate tumor suppressor genes and induce apoptosis in BCL6-dependent cancer cells. It has shown activity in B-cell lymphoma models. Detailed IC50 values and cellular activity data are available in the primary literature.
|
| ln Vivo |
In vivo, BCL6-IN-7 has been studied in animal models of B-cell lymphoma. By inhibiting BCL6, it disrupts the transcriptional repression of target genes and may induce tumor regression. Detailed in vivo efficacy data including tumor growth inhibition and biomarker modulation are available in preclinical literature. Further studies are needed to fully characterize its in vivo activity.
|
| Enzyme Assay |
In vitro binding assays for BCL6-IN-7 typically involve evaluating its inhibition of BCL6 protein-protein interactions. This is commonly measured using AlphaScreen, TR-FRET, or surface plasmon resonance (SPR) assays. The BCL6 BTB domain is incubated with a peptide representing its binding partner (e.g., SMRT or BCOR) in the presence of varying concentrations of the compound. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Cell-based assays for BCL6-IN-7 involve culturing B-cell lymphoma cell lines (e.g., DLBCL cells) in appropriate media. Cells are treated with BCL6-IN-7 at concentrations ranging from 0.01 µM to 10 µM for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assays. BCL6 target gene expression is measured by qPCR. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining.
|
| Animal Protocol |
In vivo animal experiments for BCL6-IN-7 typically involve administration to tumor-bearing mice (xenograft models of B-cell lymphoma) via oral gavage or intraperitoneal injection. Tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. BCL6 target gene expression is assessed in tumor tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters.
|
| ADME/Pharmacokinetics |
As a small molecule (molecular weight 366.8, formula C18H15ClN6O), BCL6-IN-7 has moderate lipophilicity. It is soluble in DMSO (5 mg/mL). Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. Oral bioavailability is expected based on its physicochemical properties.
|
| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for BCL6-IN-7 from the search results. As a BCL6 inhibitor, potential toxicity may include effects on germinal center B-cell function and immune response. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted. Standard laboratory safety precautions should be followed.
|
| References | |
| Additional Infomation |
BCL6-IN-7 (CAS#: 2097518-46-0) is a small molecule inhibitor targeting the BCL6 protein. It is a potent BCL6 protein-protein interaction (PPI) inhibitor. BCL6 is a transcriptional repressor involved in B-cell lymphoma. Molecular weight: 366.8, formula: C18H15ClN6O.
|
| Molecular Formula |
C18H15CLN6O
|
|---|---|
| Molecular Weight |
366.80430150032
|
| Exact Mass |
366.099
|
| CAS # |
2097518-46-0
|
| PubChem CID |
137348674
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.3
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
494
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1=CN=C(N=C1NC1C=CC2=C(C=1)CC(N2)=O)NCC1C=NC=CC=1
|
| InChi Key |
MUSYPBPUEKXCSS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H15ClN6O/c19-14-10-22-18(21-9-11-2-1-5-20-8-11)25-17(14)23-13-3-4-15-12(6-13)7-16(26)24-15/h1-6,8,10H,7,9H2,(H,24,26)(H2,21,22,23,25)
|
| Chemical Name |
5-[[5-chloro-2-(pyridin-3-ylmethylamino)pyrimidin-4-yl]amino]-1,3-dihydroindol-2-one
|
| 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 : ~5 mg/mL (~13.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7263 mL | 13.6314 mL | 27.2628 mL | |
| 5 mM | 0.5453 mL | 2.7263 mL | 5.4526 mL | |
| 10 mM | 0.2726 mL | 1.3631 mL | 2.7263 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
