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

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. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)

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SJ11646 Chemical Structure

SJ11646 Chemical Structure

CAS No. : 2933135-82-9

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SJ11646 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Lck Fyn Blk Hck Lyn Yes SRC-3

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DDR1 DDR2

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Abl Bcr-Abl

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Description

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)

Molecular Weight

746.28

Formula

C36H40ClN9O5S
CAS No.
SMILES

O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCCNC(COC4=CC=C(C(CC5)C(NC5=O)=O)C=C4)=O)CC3)=C2)S1)NC6=C(C)C=CC=C6Cl
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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SJ11646 Related Classifications

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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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