DZ-837
Based on 1 Customer Validation
DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949)[1].
(Pink: BCL6 ligand (HY-161990); Blue: Cereblon ligand (HY-103596); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 95.48%
- CAS 番号: 3105664-95-4
- 分子式: C42H44FN9O7S
- 分子量:837.92
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
BCL6[1]
|
Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DOHH-2 | IC50 |
56.2 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human DOHH-2 cells assessed as inhibition in cell growth measured after 6 days by MTS assay
Antiproliferative activity against BCL6-dependent human DOHH-2 cells assessed as inhibition in cell growth measured after 6 days by MTS assay
|
[PMID: 39208743] |
| HEK-293T | IC50 |
>10000 nM
Compound: 3d; DZ-837
|
Cytotoxicity against HEK293T cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Cytotoxicity against HEK293T cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| OCI-Ly1 | IC50 |
1370 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human OCI-Ly1 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Antiproliferative activity against BCL6-dependent human OCI-Ly1 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| SUD4 | IC50 |
399 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human SU-DHL-4 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Antiproliferative activity against BCL6-dependent human SU-DHL-4 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| SU-DHL-6 | IC50 |
450.9 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human SU-DHL-6 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Antiproliferative activity against BCL6-dependent human SU-DHL-6 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| WI-38 VA13 | IC50 |
>10000 nM
Compound: 3d; DZ-837
|
Cytotoxicity against human WI-38 VA13 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Cytotoxicity against human WI-38 VA13 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
化学情報
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CAS 番号 3105664-95-4
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性状 Solid
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分子量 837.92
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分子式 C42H44FN9O7S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(C2=CCCC2)S1)NC3=CC=C(NC4=NC(N5CCN(CCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)CC5)=NC=C4F)C=C3OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 25 mg/mL (29.84 mM; ultrasonic and heat to 60°C; 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. 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. 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)
純度とドキュメンテーション
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データシート (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 1.1934 mL | 5.9672 mL | 11.9343 mL | 29.8358 mL |
| 5 mM | 0.2387 mL | 1.1934 mL | 2.3869 mL | 5.9672 mL | |
| 10 mM | 0.1193 mL | 0.5967 mL | 1.1934 mL | 2.9836 mL | |
| 15 mM | 0.0796 mL | 0.3978 mL | 0.7956 mL | 1.9891 mL | |
| 20 mM | 0.0597 mL | 0.2984 mL | 0.5967 mL | 1.4918 mL | |
| 25 mM | 0.0477 mL | 0.2387 mL | 0.4774 mL | 1.1934 mL |