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Potent ABL and SRC family tyrosine kinases (TYKs) degrader with greater antileukemic efficacy than dasatinib in cultures and in vivo.
SJ11646 is a potent and high-affinity (LCK/ABL1/SRC Kd = 0.14/0.054/0.17 nM for SJ11646 vs. 0.09/0.054/0.19 nM for dasatinib) ABL and SRC family tyrosine kinases (TYKs) degrader composed of dasatinib linked to a E3 ligase cereblon (CRBN)-binding ligand. SJ11646 effectively degrades SRC family TYKs in KOPT-K1 cells (LCKCSKSRCFYN; 100 nM for 24h) and is 55,114-times more cytotoxic (LC50 = 0.0123 pM) than dasatinib against the BCR-ABL fusion-harboring B-ALL cell line SUP-B15. When used at equal molar amount via daily i.p.SJ11646 (15 mg/kg) shows significantly greater antileukemic efficacy than dasatinib (10 mg/kg) in two T-ALL PDX models in mice in vivo. |
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| Company Name: |
R&D Systems, Inc
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| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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