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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-TG-1701
TG-1701

Chemical Structure : TG-1701

CAS No.: 1858206-58-2

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TG-1701 (TG1701, Edralbrutinib)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 491.499
分子式 C26H23F2N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-4-Amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one

参考文献

1. Ribeiro ML, et al. Clin Cancer Res. 2021 Dec 1;27(23):6591-6601.

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