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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-TL-895
TL-895

Chemical Structure : TL-895

CAS No.: 1415823-49-2

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TL-895 (M7583, TL895)

货号: PC-21379Not For Human Use, Lab Use Only.

TL-895 (M7583) is a potent, highly selective, ATP-competitive, second-generation, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with biochemical IC50 of 1.5 nM.

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥3980 In stock
50 mg ￥5680 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TL-895 (M7583) is a potent, highly selective, ATP-competitive, second-generation, irreversible inhibitor of Bruton's tyrosine kinase (BTK) with biochemical IC50 of 1.5 nM.
TL-895 (M7583) has an average IC50 of 18.5 nM for BTK against Millipore Kinase Profiler screening panel, profiling across 270 protein kinases at 1 μM, only 3 additional kinases are also inhibited by TL-895 (Blk, BMX, and Txk) with IC50 values of 77, 5, and 62 nM, respectively.
TL-895 (M7583) inhibits BTK auto-phosphorylation at Y223 after BCR stimulation with anti-IgM in the human Burkitt's lymphoma B-cell line Ramos with IC50 of 1-10 nM.
TL-895 (M7583) inhibits growth of primary CLL blasts in vitro with IC50 of 0.2 uM, similar to ibrutinib and acalabrutinib.
TL-895 (M7583) inhibits the ADCC mechanism of therapeutic antibodies only at supra-clinical exposure levels.
TL-895 (M7583) significantly inhibits tumor growth in the Mino MCL xenograft model and in 5/21 DLBCL PDX models relative to vehicle controls.

物理化学性质&存储条件

分子量 447.51
分子式 C25H26FN5O2
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

1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)-4-fluoropiperidin-1-yl)prop-2-en-1-one

参考文献

1. Goodstal SM, et al. Sci Rep. 2023 Nov 21;13(1):20412.

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