1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs RET
  3. PROTAC RET Degrader 1

PROTAC RET Degrader 1 (Compound 20) 是一种口服有效且能穿过血脑屏障的 RET PROTAC 降解剂,其对于 RET (WT)RET (G810S)RET (G810C)RET (G810R)DC50 值分别为 1.7、3、12 和 21 nM。PROTAC RET Degrader 1 在携带致癌 RET 融合 (如 KIF5B-RET、CCDC6-RET) 或突变 (如RET (C634W)) 的癌细胞系 (如 Ba/F3、LC-2/ad、TT 细胞) 中具有强效抗增殖活性。PROTAC RET Degrader 1 在人源肿瘤异体移植 (PDX) 小鼠模型具有显著的抗肿瘤活性。PROTAC RET Degrader 1 可用于研究 RET 阳性癌症 (粉色:RET 配体 (HY-179308);蓝色:CRBN 配体 (HY-179307);黑色:连接子)。

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PROTAC RET Degrader 1

PROTAC RET Degrader 1 Chemical Structure

CAS No. : 2760847-82-1

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  • 生物活性

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生物活性

PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker)[1].

IC50 & Target[1]

Cereblon

 

分子量

869.04

Formula

C48H57FN12O3

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.

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参考文献
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  • 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 RET Degrader 1
目录号:
HY-178964
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