2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Bcr-Abl
  4. P22D

P22D 是一种基于 Dasatinib (HY-10181) 的 BCR-ABL PROTAC 降解剂，其对于野生型 BCR-ABL 蛋白的 DC50 约为 10 nM。P22D 无法降解 BCR-ABL T315I 突变体。P22D 对 K562 细胞 (野生型) 具有抑制活性，对 BaF3-BCR-ABL (T315I) 细胞无效。P22D 可用于研究慢性髓系白血病。
(粉色: Target Protein Ligand-Linker Conjugates 配体 (HY-107447)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子 (HY-180980))。

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P22D

P22D Chemical Structure

CAS No. : 2635386-51-3

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P22D 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Abl Bcr-Abl

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia[1]. (Pink: Target Protein Ligand-Linker Conjugates ligand (HY-107447); Blue: Cereblon ligand (HY-14658); Black: linker (HY-180980)).

IC50 & Target[1]

Bcr-AblWT

10 nM (DC50)

Cereblon

 

分子量

1056.58

Formula

C49H58ClN13O10S
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

P22D 相关分类

  • 摩尔计算器

  • 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.

Keywords:

P22D2635386-51-3PROTACsBcr-AblPROTACBCR-ABLdrug resistanceT315I mutantprotein degradationdasatinibCRBN E3 ligaseInhibitorinhibitorinhibit

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目录号：
HY-180979
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