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COA of TG-1701

Description:

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.

Chemical Information

Catalog Novel inhibitors
CAS 1858206-58-2
Molecular Weight (MW) 491.499
Molecular Formula C26H23F2N5O3
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Handling:

Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.