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AVL-292 besylate

Chemical Structure : AVL-292 besylate

CAS No.: 1360053-81-1

AVL-292 besylate (Spebrutinib besylate, CC-292 besylate)

Catalog No.: PC-45402Not For Human Use, Lab Use Only.

AVL-292 besylate (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM.

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Biological Activity

AVL-292 besylate (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM.
AVL-292 besylate (Spebrutinib, CC-292) also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 uM, 2.43 uM, 4.4 uM, and 7.15 uM, rspectively.
AVL-292 besylate (Spebrutinib, CC-292) shows anti-inflammatory activity in the collagen-induced arthritis model of autoimmune disease.
AVL-292 besylate (Spebrutinib, CC-292) also prevents NRG- and EGF-dependent growth factor-driven resistance to lapatinib in HER2(+) breast cancer cells.

Physicochemical Properties

M.Wt 581.6152
Formula C28H28FN5O6S
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

2-Propenamide, N-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-, benzenesulfonate (1:1)

References

1. Evans EK, et al. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28.

2. Eda H, et al. Leukemia. 2014 Sep;28(9):1892-901.

3. Wang X, et al. Mol Cancer Ther. 2016 Sep;15(9):2198-208.

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