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. [1][2]. Pink: LCK ligand (HY-107447) ; Blue: CRBN ligase ligand (HY-163169) ; Black: linker (HY-76667)

Product Specifications

CAS Number

[2933135-82-9]

UNSPSC

12352005

Target

Apoptosis; Bcr-Abl; Discoidin Domain Receptor; PROTACs; Src

Related Pathways

Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

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

Molecular Formula

C36H40ClN9O5S

Molecular Weight

746.28

References & Citations

[1]Yang JJ, et al. LCK-targeting molecular glues overcome resistance to inhibitor-based therapy in T-cell acute lymphoblastic leukemia. bioRxiv [Preprint]. 2025 Jul 7:2025.07.03.663042.|[2]Hu J, et al. Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia. Sci Transl Med. 2022 Aug 24;14 (659) :eabo5228.