2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Bcr-Abl
  4. P19P

P19P 是一种基于 Ponatinib (HY-12047) 的 BCR-ABL PROTAC 降解剂，其对于野生型 BCR-ABL 蛋白的 DC50 约为 20 nM。P19P 能够有效降解 T315I、E255K、H396R 和 V468F 等多种耐药突变体，在 BaF3-BCR-ABL (T315I) 细胞上表现了强效的抗增殖活性。P19P 对 ABL (T315I) 保持了强效抑制活性，其 IC50 为 13.1 nM。P19P 不抑制 HUVEC 的管腔形成。P19P 可用于研究慢性髓系白血病和急性淋巴细胞白血病。
(粉色: Bcr-Abl 配体 (HY-12047)；蓝色: Ligands for E3 Ligase 配体 (HY-14658)；黑色: 连接子 (HY-180978))。

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P19P

P19P Chemical Structure

CAS No. : 2512843-74-0

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P19P 相关抗体

Top Publications Citing Use of Products

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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

P19P is a BCR-ABL PROTAC degrader based on Ponatinib (HY-12047), with a DC50 value of approximately 20 nM for the wild-type BCR-ABL protein. P19P can effectively degrade various drug-resistant mutants such as T315I, E255K, H396R, and V468F, and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19P maintains strong inhibitory activity against ABL (T315I), with a IC50 of 13.1 nM. P19P does not inhibit the formation of vascular lumens in HUVEC. P19P can be used for research on chronic myeloid leukemia and acute lymphoblastic leukemia[1]. (Pink: Bcr-Abl ligand (HY-12047); Blue: Ligands for E3 Ligase ligand (HY-14658); Black: linker (HY-180978)).

IC50 & Target[1]

Bcr-AblWT

20 nM (DC50)

Cereblon

 

分子量

1087.11

Formula

C55H57F3N12O9
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

P19P 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:

P19P2512843-74-0PROTACsBcr-AblPROTACBCR-ABLPonatinibT315I mutantprotein degradationdrug resistanceadverse effectsCRBN E3 ligaseInhibitorinhibitorinhibit

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目录号：
HY-180977
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