1. PROTAC Immunology/Inflammation
  2. PROTACs BCL6 IKZF Family
  3. PROTAC BCL6/IKZF1/3 Degrader-1

PROTAC BCL6/IKZF1/3 Degrader-1 是一种选择性且具有口服活性的 BCL6IKZF1/3 PROTAC 降解剂。PROTAC BCL6/IKZF1/3 Degrader-1 在各种生发中心 B 细胞样 (GCB) 和活化 B 细胞样 (ABC) 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞系中表现出优异的抗增殖效果。PROTAC BCL6/IKZF1/3 Degrader-1 可用于癌症研究,如淋巴瘤。(结构:粉色:BCL6/IKZF1/3 配体 (HY-179064);蓝色:CRBN 连接酶配体 (HY-41547);黑色:连接子 (HY-42427);CRBN 配体-Linker: (HY-179066))

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PROTAC BCL6/IKZF1/3 Degrader-1

PROTAC BCL6/IKZF1/3 Degrader-1 Chemical Structure

1.  客户无需承担相应的运输费用。

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查看 PROTACs 亚型特异性产品:

查看 IKZF Family 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BCL6/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BCL6/IKZF1/3 Degrader-1 exhibits superior antiproliferative effects in various germinal center B-cell-like (GCB) and activated B-cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cell lines. PROTAC BCL6/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma[1]. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179064); Blue: CRBN ligand (HY-41547); Black: linker (HY-42427); CRBN ligand-Linker: (HY-179066))

IC50 & Target[1]

IKZF1

 

IKZF3

 

Cereblon

 

体外研究
(In Vitro)

PROTAC BCL6/IKZF1/3 Degrader-1 (Compound BC6) (0.03-100 nM, 24 h) 在 OCI-ly1、OCI-ly10、SU-DHL4 等 GCB/ABC 亚型弥漫大 B 细胞淋巴瘤 (DLBCL) 细胞中,特异性降解 BCL6 (DC50 值为 0.08-1.04 nM)、IKZF1 (DC50 值为 5.74-26.32 nM) 和 IKZF3 蛋白 (DC50 值为 1.05-6.40 nM)[1]
PROTAC BCL6/IKZF1/3 Degrader-1 (0.03-100 nM, 24 h) 可显著抑制 OCI-ly1、OCI-ly10 和 SU-DHL4 细胞的增殖,其 IC50 值为 0.46-35.68 nM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PROTAC BCL6/IKZF1/3 Degrader-1 (Compound BC6) (25-50 mg/kg,口服,每日一次,连续 21 天) 在携带 OCI-ly1 异种移植物的 NOD-SCID 小鼠中显著抑制肿瘤生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old female NOD-SCID mice bearing OCI-ly1 xenografts[1]
Dosage: 25 and 50 mg/kg
Administration: Orally administration, daily for 21 days
Result: Showed tumor growth inhibition (TGI) rates of 63.55% and 72.23%.
Reduced tumor weight.
Degraded BCL6 and IKZF1/3 proteins in tumor tissues.
Showed no significant body weight changes.
分子量

853.36

Formula

C43H49ClN10O7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PROTAC BCL6/IKZF1/3 Degrader-1
目录号:
HY-179075
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