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製品番号: HY-146184

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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 番号: 2378853-67-7
分子式: C₂₆H₂₉ClF₂N₆O₃
分子量:547.00

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (282 KB)

CCT373567 構造式

CAS 番号: 2378853-67-7

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Cellular Effect

Cell Line	Type	Value	Description	References
OCI-Ly1	DC₅₀	>2000 nM	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.	35653645
KARPAS-422	DC₅₀	>2000 nM	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.	35653645
OCI-Ly1	GI50	83 nM	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.	35653645
KARPAS-422	GI50	38 nM	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.	35653645
HT	GI50	362 nM	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.	35653645
SU-DHL-4	GI50	820 nM	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.	35653645
OCI-Ly3	GI50	2145 nM	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.	35653645

体外実験

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.

化学情報

CAS 番号 2378853-67-7
分子量 547.00
分子式 C₂₆H₂₉ClF₂N₆O₃
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (282 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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