| Size | Price | Stock | Qty |
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| Targets |
BCL6 (transcriptional repressor). CCT-373566 is a potent and orally active degrader of BCL6 with a DC50 (concentration for 50% degradation) of 2.2 nM (or 0.7 nM by more potent estimates). It induces sustained depletion of BCL6 protein via the ubiquitin-proteasome pathway, leading to antiproliferative effects in BCL6-dependent cancer cells. The compound shows selectivity for BCL6 degradation over other targets.
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| ln Vitro |
CCT-373566 (CCT373566) displays potent antiproliferation efficacy in vitro in a panel of BCL6-dependent cell lines including lymphoma cells. The degrader shows stronger antiproliferative activity compared to a non-degrading BCL6 inhibitor (CCT373567). CCT-373566 is effective at low nanomolar concentrations due to its degradation mechanism, achieving sustained target depletion.
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| ln Vivo |
CCT-373566 reduces tumor growth in vivo and showed modest in vivo efficacy in a lymphoma xenograft mouse model following oral dosing. The compound is orally bioactive and suitable for sustained depletion of BCL6 in vivo. Further details of in vivo efficacy are available in the primary literature.
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| Enzyme Assay |
Not explicitly detailed in reference sources. A typical BCL6 degradation assay uses a HiBiT knock-in system or Western blot to measure BCL6 protein levels in cells treated with CCT-373566 for 4-24 hours. The DC50 is determined from dose-response curves, and degradation kinetics are assessed over time. The compound is incubated with recombinant BCL6 and components of the ubiquitination machinery to confirm targeted degradation.
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| Cell Assay |
Cells (e.g., lymphoma cell lines) are treated with CCT-373566 at various concentrations (0.1-1000 nM) for 24-72 hours, and cell viability is measured using CellTiter-Glo or MTT assay to determine the GI50. For degradation assessment, cells are treated with CCT-373566 for 6-24 hours and lysed for Western blot analysis of BCL6 protein levels.
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| Animal Protocol |
In lymphoma xenograft mouse models, CCT-373566 is administered orally at doses ranging from 1-30 mg/kg daily or twice daily. Tumor volumes are measured twice weekly, and tumor regression is assessed at the end of the study. BCL6 protein levels in tumor tissues are measured to confirm target degradation. Pharmacodynamic studies assess the duration of BCL6 suppression following oral dosing.
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| ADME/Pharmacokinetics |
CCT-373566 is orally bioavailable with a molecular weight of 547.00 and formula C26H29ClF2N6O3. It is soluble in DMSO (50 mg/mL, 91.41 mM). Storage should be at 4degC protected from light, with powder stable for up to 3 years at -20degC. In solution at -80degC, it is stable for 6 months. For in vivo studies, it can be formulated in appropriate vehicles for oral administration.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for CCT-373566 are provided in the reference sources. In the lymphoma xenograft mouse model, oral dosing of CCT-373566 is reported to be tolerated, but comprehensive safety studies are needed. The compound is for research use only and not intended for human consumption.
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| References | |
| Additional Infomation |
This BCL6 degrader represents a novel therapeutic approach for BCL6-driven lymphomas and potentially other BCL6-dependent malignancies. CCT-373566 is a research compound in preclinical development and is not yet approved for clinical use. It has been developed as a first-in-class orally bioavailable BCL6 degrader with high potency and sustained target depletion.
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| Molecular Formula |
C26H29CLF2N6O3
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|---|---|
| Molecular Weight |
547.00
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| Exact Mass |
546.2
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| Elemental Analysis |
C, 57.09; H, 5.34; Cl, 6.48; F, 6.95; N, 15.36; O, 8.77
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| CAS # |
2378853-66-6
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| PubChem CID |
146189160
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
38
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| Complexity |
954
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@H]1C[C@H](CN(C1)C2=NC=C(C(=N2)NC3=CC4=C(C=C3)N(C(=O)C5=C4N[C@H](C(CO5)(F)F)C6CC6)C)Cl)O
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| InChi Key |
GSGDUDAFETZSPM-IATAILRESA-N
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| InChi Code |
InChI=1S/C26H29ClF2N6O3/c1-13-7-16(36)11-35(10-13)25-30-9-18(27)23(33-25)31-15-5-6-19-17(8-15)20-21(24(37)34(19)2)38-12-26(28,29)22(32-20)14-3-4-14/h5-6,8-9,13-14,16,22,32,36H,3-4,7,10-12H2,1-2H3,(H,30,31,33)/t13-,16+,22-/m0/s1
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| Chemical Name |
(2S)-10-[[5-chloro-2-[(3R,5S)-3-hydroxy-5-methylpiperidin-1-yl]pyrimidin-4-yl]amino]-2-cyclopropyl-3,3-difluoro-7-methyl-2,4-dihydro-1H-[1,4]oxazepino[2,3-c]quinolin-6-one
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| Synonyms |
CCT373566; CCT 373566; CCT-373566;
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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 : ~50 mg/mL (~91.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 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 25.0 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 | 1.8282 mL | 9.1408 mL | 18.2815 mL | |
| 5 mM | 0.3656 mL | 1.8282 mL | 3.6563 mL | |
| 10 mM | 0.1828 mL | 0.9141 mL | 1.8282 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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