CCT373567
CCT373567 is a non-degrading isomer of the BCL6 degrader CCT373566 (HY-146185). CCT373567 acts as a BCL6 inhibitor with an IC50 of 2.9 nM. CCT373567 exerts growth inhibitory activity against cancer cells expressing BCL6, but shows low activity against cancer cells with low BCL6 expression. CCT373567 can be used in research related to diffuse large B-cell lymphoma.
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- CAS No.: 2378853-67-7
- Formule: C26H29ClF2N6O3
- Masse moléculaire:547.00
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| OCI-Ly1 | DC50 |
>2000 nM
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BCL6 degradation induction in human OCI-Ly1 diffuse large B-cell lymphoma cells measured by MSD BCL6 degrader cell-based assay.
BCL6 degradation induction in human OCI-Ly1 diffuse large B-cell lymphoma cells measured by MSD BCL6 degrader cell-based assay.
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35653645 |
| KARPAS-422 | DC50 |
>2000 nM
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BCL6 degradation induction in human Karpas 422 diffuse large B-cell lymphoma cells measured by MSD BCL6 degrader cell-based assay.
BCL6 degradation induction in human Karpas 422 diffuse large B-cell lymphoma cells measured by MSD BCL6 degrader cell-based assay.
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35653645 |
| OCI-Ly1 | GI50 |
83 nM
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Antiproliferative activity against human OCI-Ly1 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
Antiproliferative activity against human OCI-Ly1 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
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35653645 |
| KARPAS-422 | GI50 |
38 nM
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Antiproliferative activity against human Karpas 422 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
Antiproliferative activity against human Karpas 422 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
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35653645 |
| HT | GI50 |
362 nM
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Antiproliferative activity against human HT diffuse large B-cell lymphoma cells measured by cell proliferation assay.
Antiproliferative activity against human HT diffuse large B-cell lymphoma cells measured by cell proliferation assay.
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35653645 |
| SU-DHL-4 | GI50 |
820 nM
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Antiproliferative activity against human SU-DHL-4 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
Antiproliferative activity against human SU-DHL-4 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
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35653645 |
| OCI-Ly3 | GI50 |
2145 nM
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Antiproliferative activity against human OCI-Ly3 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
Antiproliferative activity against human OCI-Ly3 diffuse large B-cell lymphoma cells measured by cell proliferation assay.
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35653645 |
In Vitro
CCT373567 potently inhibits BCL6 BTB domain-corepressor interactions in a cell-free TR-FRET assay with an IC50 of 2.9 nM[1].
CCT373567 fails to induce meaningful BCL6 degradation in OCI-Ly1 cells, with a DC50 >2000 nM and a maximum degradation of >30%[1].
CCT373567 inhibits proliferation of BCL6-expressing diffuse large B-cell lymphoma cell lines (OCI-Ly1, Karpas 422, HT, SU-DHL-4) with GI50 values ranging from 38 nM to 820 nM, and shows weak activity against low BCL6-expressing OCI-Ly3 cells with a GI50 of 2145 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2378853-67-7
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Masse moléculaire 547.00
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Formule C26H29ClF2N6O3
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCT373567 Related Classifications
HY-146184 Related Classifications
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