2933135-82-9
Chemical Structure
SJ11646
- CAS No.: 2933135-82-9
- Formula:C36H40ClN9O5S
- Molecular Weight:746.28
IUPAC Name: N-(2-chloro-6-methylphenyl)-2-((6-(4-(3-(2-(4-(2,6-dioxopiperidin-3-yl)phenoxy)acetamido)propyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide
InChIKey: AJNQGWOQPRWRML-UHFFFAOYSA-N
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
Biological Activity: SJ11646 is a LCK PROTAC degrader with a DC50 value of 0.00838 pM against LCK. SJ11646 recruits CRBN and LCK to form a ternary complex, inducing cereblon-mediated proteasomal degradation of LCK. SJ11646 induces cytotoxicity in T-ALL cells, but such cytotoxicity is reduced in cells harboring the LCKT316I mutation. SJ11646 can be used in studies related to T-cell acute lymphoblastic leukemia[1][2].
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SJ11646 | 99.3% | SJ11646 is a LCK PROTAC degrader with a DC50 value of 0.00838 pM against LCK. SJ11646 recruits CRBN and LCK to form a ternary complex, inducing cereblon-mediated proteasomal degradation of LCK. SJ11646 induces cytotoxicity in T-ALL cells, but such cytotoxicity is reduced in cells harboring the LCKT316I mutation. SJ11646 can be used in studies related to T-cell acute lymphoblastic leukemia. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Hu J, et al. Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia. Science translational medicine. 2022 Aug 24;14(659):eabo5228. [Content Brief]
Keywords