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Chemical Structure : TG-1701
Catalog No.: PC-72430Not For Human Use, Lab Use Only.
TG-1701 (Edralbrutinib, TG1701) is a irreversible, orally available, potent and highly specific BTK inhibitor with Kd of 3 nM, IC50 of 6.7 nM, more selective than ibrutinib.
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TG-1701 (Edralbrutinib, TG1701) is a irreversible, orally available, potent and highly specific BTK inhibitor with Kd of 3 nM, IC50 of 6.7 nM, more selective than ibrutinib.
TG-1701 exerts similar activity than the first-in-class BTKi ibrutinib, although with greater selectivity, in in vitro and in vivo models of B-NHL.
TG-1701 impaired BCR downstream signaling in a concentration-dependent manner in IgM-stimulated cells, with maximal effects observed at 100 nM for TG-1701.
TG-1701 shows mean GI50 of 6.4 uM in a set of 10 parental B-NHL cell lines (MCL cell lines GI50=4.3 uM).
TG-1701 blunts Ikaros gene signature, including YES1 and MYC, in early-responder patients as well as in BTKi-sensitive B-NHL cell lines and xenografts.
| M.Wt | 491.499 | |
| Formula | C26H23F2N5O3 | |
| Appearance | Solid | |
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1. Ribeiro ML, et al. Clin Cancer Res. 2021 Dec 1;27(23):6591-6601.
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