2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs Src Discoidin Domain Receptor Bcr-Abl Apoptosis
  4. SJ11646

SJ11646 是一种基于 Dasatinib (HY-10181) 的 LCK PROTAC 降解剂，其 DC50 为 0.00838 pM。SJ11646 对 LCK 激活的 T 细胞急性淋巴细胞白血病 (T-ALL) 细胞和原发性白血病样本具有强效细胞毒性，可显著延长 LCK 信号抑制时间，并诱导 T-ALL 细胞凋亡 (apoptosis)。SJ11646 可与 51 种人类激酶 (尤其是 ABL1、KIT 和 DDR1) 高亲和力结合。SJ11646 在 T-ALL 小鼠模型中表现出卓越的抗白血病疗效。粉色：LCK ligand (HY-107447)；蓝色：CRBN ligase ligand (HY-163169)；黑色：linker (HY-76667)

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SJ11646

SJ11646 Chemical Structure

CAS No. : 2933135-82-9

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SJ11646 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Src 亚型特异性产品:

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Lck Fyn Blk Hck Lyn Yes SRC-3

查看 Discoidin Domain Receptor 亚型特异性产品:

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DDR1 DDR2

查看 Bcr-Abl 亚型特异性产品:

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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

SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. [1][2]. Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)

IC50 & Target[2]

DDR1

 

Abl1

 

Lck

0.00838 pM (DC50)

分子量

746.28

Formula

C36H40ClN9O5S
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

SJ11646 相关分类

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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.

Keywords:

SJ116462933135-82-9SJ 11646SJ-11646PROTACsSrcDiscoidin Domain ReceptorBcr-AblApoptosisPROTACDegradationLCKAntileukemicT-cell acute lymphoblastic leukemiaT-ALLKOPT-K1 cellsJurkat cellsT-ALL mice modelInhibitorinhibitorinhibit

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