CCT373566
Based on 1 Customer Validation
CCT373566 is an orally active BCL6 Molecular glue degrader with a DC50 of 0.7 nM. CCT373566 induces proteasomal degradation of BCL6 by promoting the formation of higher-order BCL6 complexes recognizable by E3 ligases. CCT373566 reduces tumor growth in lymphoma xenograft models. CCT373566 can be used in research related to diffuse large B-cell lymphoma.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.61%
- CAS 番号: 2378853-66-6
- 分子式: C26H29ClF2N6O3
- 分子量:547.00
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| OCI-Ly1 | DC50 |
0.7 nM
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Induction of BCL6 degradation in OCI-Ly1 diffuse large B-cell lymphoma cells measured by MSD BCL6 degradation cell-based assay.
Induction of BCL6 degradation in OCI-Ly1 diffuse large B-cell lymphoma cells measured by MSD BCL6 degradation cell-based assay.
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35653645 |
| OCI-Ly1 | DC50 |
0.088 nM
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Calculated free induction of BCL6 degradation in OCI-Ly1 diffuse large B-cell lymphoma cells measured by MSD BCL6 degradation cell-based assay.
Calculated free induction of BCL6 degradation in OCI-Ly1 diffuse large B-cell lymphoma cells measured by MSD BCL6 degradation cell-based assay.
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35653645 |
| KARPAS-422 | DC50 |
1.0 nM
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Induction of BCL6 degradation in Karpas 422 diffuse large B-cell lymphoma cells measured by MSD BCL6 degradation cell-based assay.
Induction of BCL6 degradation in Karpas 422 diffuse large B-cell lymphoma cells measured by MSD BCL6 degradation cell-based assay.
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35653645 |
| OCI-Ly1 | GI50 |
2.1 nM
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Antiproliferative activity against OCI-Ly1 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
Antiproliferative activity against OCI-Ly1 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
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35653645 |
| KARPAS-422 | GI50 |
1.4 nM
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Antiproliferative activity against Karpas 422 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
Antiproliferative activity against Karpas 422 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
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35653645 |
| HT | GI50 |
8.0 nM
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Antiproliferative activity against HT diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
Antiproliferative activity against HT diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
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35653645 |
| SU-DHL-4 | GI50 |
12.5 nM
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Antiproliferative activity against SU-DHL-4 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
Antiproliferative activity against SU-DHL-4 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
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35653645 |
| OCI-Ly3 | GI50 |
1900 nM
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Antiproliferative activity against BCL6-low OCI-Ly3 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
Antiproliferative activity against BCL6-low OCI-Ly3 diffuse large B-cell lymphoma cells assessed as inhibition of cell growth incubated for 14 days by 14-day cell proliferation assay.
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35653645 |
体外実験
CCT373566 potently inhibits BCL6 BTB domain peptide binding in a cell-free TR-FRET assay with an IC50 of 2.2 nM[1].
CCT373566 (1 μM) demonstrates selective activity with minimal off-target interactions when profiled against 468 kinases and 78 safety panel targets[1].
CCT373566 potently inhibits BCL6 in a cell-free TR-FRET assay with an IC50 of 2.2 nM[2].
CCT373566 induces complete BCL6 degradation in OCI-Ly1 diffuse large B-cell lymphoma cells with a DC50 of 0.7 nM and a calculated free DC50 of 0.088 nM[1].
CCT373566 induces 85% BCL6 degradation in Karpas 422 diffuse large B-cell lymphoma cells with a DC50 of 1.0 nM[1].
CCT373566 potently inhibits the proliferation of OCI-Ly1 diffuse large B-cell lymphoma cells with a GI50 of 2.1 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
体内実験
CCT373566 (50 mg/kg; p.o.; twice daily; 22 days) achieves modest tumor growth inhibition (T/C = 0.6) in an HT DLBCL xenograft model while sustaining tumor BCL6 depletion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (female, subcutaneous xenograft of OCI-Ly1 cells, dosing initiated 20 days post-injection when tumors reached 0.5-0.8 cm3)[1]
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Dosage:50 mg/kg
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Administration:p.o.; single dose
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Result:Decreased tumor BCL6 levels significantly at 12, 16, and 24 hours post-dosing compared to vehicle-treated controls.
Sustained mean free plasma concentrations above the calculated free DC50 (0.09 nM) for 24 hours post-dosing.
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Animal Model:SCID mice (female, subcutaneous xenograft of HT cells, dosing initiated 20 days post-injection when tumors reached 0.5-0.8 cm3)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily; 22 days
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Result:Achieved tumor growth inhibition with a T/C ratio of 0.6 compared to vehicle-treated controls after 22 days.
Caused no body weight loss.
Decreased tumor BCL6 levels 4 and 12 hours after the final dose.
化学情報
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CAS 番号 2378853-66-6
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性状 Solid
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分子量 547.00
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分子式 C26H29ClF2N6O3
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Color Light yellow to yellow
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SMILES
O=C1N(C)C2=C(C=C(NC3=NC(N4C[C@H](O)C[C@H](C)C4)=NC=C3Cl)C=C2)C5=C1OCC(F)(F)[C@H](C6CC6)N5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (91.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
純度とドキュメンテーション
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データシート (288 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Huckvale R, et al. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 . Journal of medicinal chemistry. 2022 Jun 23;65(12):8191-8207. [Content Brief]
[2]. Harnden AC, et al. Discovery of an Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones. Journal of medicinal chemistry. 2023 Apr 27;66(8):5892-5906. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8282 mL | 9.1408 mL | 18.2815 mL | 45.7038 mL |
| 5 mM | 0.3656 mL | 1.8282 mL | 3.6563 mL | 9.1408 mL | |
| 10 mM | 0.1828 mL | 0.9141 mL | 1.8282 mL | 4.5704 mL | |
| 15 mM | 0.1219 mL | 0.6094 mL | 1.2188 mL | 3.0469 mL | |
| 20 mM | 0.0914 mL | 0.4570 mL | 0.9141 mL | 2.2852 mL | |
| 25 mM | 0.0731 mL | 0.3656 mL | 0.7313 mL | 1.8282 mL | |
| 30 mM | 0.0609 mL | 0.3047 mL | 0.6094 mL | 1.5235 mL | |
| 40 mM | 0.0457 mL | 0.2285 mL | 0.4570 mL | 1.1426 mL | |
| 50 mM | 0.0366 mL | 0.1828 mL | 0.3656 mL | 0.9141 mL | |
| 60 mM | 0.0305 mL | 0.1523 mL | 0.3047 mL | 0.7617 mL | |
| 80 mM | 0.0229 mL | 0.1143 mL | 0.2285 mL | 0.5713 mL |
CCT373566 関連分類
HY-146185 関連分類
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