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| Targets |
BCL6[1]
BCL6 (B-cell lymphoma 6). BCL6-IN-6 is a potent inhibitor of the transcriptional repressor BCL6. It blocks the interaction of BCL6 with its corepressors, which prevents BCL6 from repressing its target genes. This reactivation of BCL6 target genes is the mechanism by which the compound exerts its anti-lymphoma effects. |
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| ln Vitro |
BCL6-IN-6 is a potent inhibitor of BCL6 that significantly blocks its interaction with corepressors and reactivates BCL6 target genes in a dose-dependent manner. This activity makes it a promising compound for the research of B-cell malignancies, particularly diffuse large B-cell lymphoma (DLBCL).
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| ln Vivo |
In vivo, BCL6-IN-6 is used to study the role of BCL6 in lymphoma and other cancers. By inhibiting BCL6, the compound can reactivate tumor suppressor genes that are normally silenced by this transcriptional repressor. Its efficacy would be assessed in animal models of DLBCL and other BCL6-driven malignancies.
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| Enzyme Assay |
The in vitro activity of BCL6-IN-6 is typically assessed using biochemical assays that measure its ability to disrupt the BCL6-corepressor interaction. These assays often use purified BCL6 protein and a peptide representing the corepressor binding site. The compound's ability to inhibit this interaction is measured, confirming its mechanism of action.
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| Cell Assay |
Cellular assays for BCL6-IN-6 involve treating BCL6-dependent lymphoma cell lines with the compound and measuring the reactivation of BCL6 target genes. This is typically done by qPCR or RNA-seq to assess changes in gene expression. The compound's ability to inhibit cell proliferation and induce apoptosis in these cells is also measured to confirm its anti-lymphoma activity.
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| Animal Protocol |
In vivo efficacy of BCL6-IN-6 is evaluated in mouse models of DLBCL or other BCL6-driven cancers. The compound is administered to tumor-bearing mice, and its effects on tumor growth, survival, and the expression of BCL6 target genes are assessed. This helps to validate the therapeutic potential of BCL6 inhibition.
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| ADME/Pharmacokinetics |
BCL6-IN-6 is a small molecule with the molecular formula C27H31FN6O2S and a molecular weight of 522.64. Its pharmacokinetic properties, such as oral bioavailability, would be key factors for its in vivo efficacy. As a research compound, its potency and selectivity for BCL6 are its primary characteristics.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for BCL6-IN-6. As an inhibitor of a key transcriptional regulator, its safety profile would be an important consideration. Potential toxicities could be related to the reactivation of BCL6 target genes in normal tissues. Standard preclinical toxicology studies would be required to assess its safety.
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| References | |
| Additional Infomation |
BCL6-IN-6 (CAS#: 2408882-54-0) is a potent and selective inhibitor of the BCL6 transcriptional repressor. It blocks BCL6-corepressor interactions and reactivates BCL6 target genes. It is a research tool for studying BCL6-driven cancers, particularly DLBCL. It is not approved for clinical use.
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| Molecular Formula |
C27H31FN6O2S
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|---|---|
| Molecular Weight |
522.637447595596
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| Exact Mass |
522.221
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| CAS # |
2408882-54-0
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| PubChem CID |
155549001
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
810
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S1C(C(NC2C=CC(=CC=2OC)NC2=C(C=NC(=N2)N2C[C@@H](C)N[C@@H](C)C2)F)=O)=CC=C1C1=CCCC1
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| InChi Key |
VJFKSXHAFLCLLP-CALCHBBNSA-N
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| InChi Code |
InChI=1S/C27H31FN6O2S/c1-16-14-34(15-17(2)30-16)27-29-13-20(28)25(33-27)31-19-8-9-21(22(12-19)36-3)32-26(35)24-11-10-23(37-24)18-6-4-5-7-18/h6,8-13,16-17,30H,4-5,7,14-15H2,1-3H3,(H,32,35)(H,29,31,33)/t16-,17+
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| Chemical Name |
5-(cyclopenten-1-yl)-N-[4-[[2-[(3S,5R)-3,5-dimethylpiperazin-1-yl]-5-fluoropyrimidin-4-yl]amino]-2-methoxyphenyl]thiophene-2-carboxamide
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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: ≥ 4 mg/mL (7.65 mM)
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| 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 | 1.9134 mL | 9.5668 mL | 19.1336 mL | |
| 5 mM | 0.3827 mL | 1.9134 mL | 3.8267 mL | |
| 10 mM | 0.1913 mL | 0.9567 mL | 1.9134 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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