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TL-895

Chemical Structure : TL-895

CAS No.: 1415823-49-2

TL-895 (M7583, TL895)

Catalog No.: 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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 447.51
Formula C25H26FN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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