1. PROTAC Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. PROTACs Btk IKZF Family
  3. PROTAC BTK/IKZF1/3 Degrader-1

PROTAC BTK/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 BTK/IKZF1/3 Degrader-1 具有抗肿瘤活性。PROTAC BTK/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-179076);蓝色:CRBN 连接酶配体 (HY-41547))

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PROTAC BTK/IKZF1/3 Degrader-1

PROTAC BTK/IKZF1/3 Degrader-1 Chemical Structure

CAS No. : 2416130-49-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma[1]. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))

IC50 & Target[1]

IKZF1

 

IKZF3

 

Cereblon

 

体外研究
(In Vitro)

PROTAC BTK/IKZF1/3 Degrader-1 (Compound BT6) (1-300 nM, 24 h) 在 Mino 细胞、OCI-ly10 等弥漫大 B 细胞淋巴瘤 (DLBCL) 细胞中,浓度依赖性降解 BTK 和 IKZF1/3 蛋白 (BTK 在 33.3 nM 时降解率超 75%,IKZF1/3 在 300 nM 时降解率超 50%)[1]

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

体内研究
(In Vivo)

PROTAC BTK/IKZF1/3 Degrader-1 (Compound BT6) (3-10 mg/kg,口服,每日一次,连续 21 天) 在携带 OCI-ly10 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: 3 and 10 mg/kg
Administration: Orally administration, daily for 21 days
Result: Showed tumor growth inhibition (TGI) rates of 95.54% and 115.72%.
Degraded BTK and IKZF1/3 proteins in tumor tissues.
Showed no significant body weight changes.
分子量

817.94

Formula

C43H51N11O6

CAS 号
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
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  • 稀释计算器

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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 BTK/IKZF1/3 Degrader-1
目录号:
HY-179077
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