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Rocbrutinib

Chemical Structure : Rocbrutinib

CAS No.: 2485861-07-0

Rocbrutinib (LP-168, LP168)

Catalog No.: PC-23081Not For Human Use, Lab Use Only.

Rocbrutinib (LP-168) is a potent, highly selective, orally available next-generation inhibitor of Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 0.11 nM against wild-type BTK and IC50 of 1.0 nM against C481S-mutated BTK.

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

Biological Activity

Rocbrutinib (LP-168) is a potent, highly selective, orally available next-generation inhibitor of Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 0.11 nM against wild-type BTK and IC50 of 1.0 nM against C481S-mutated BTK.
Rocbrutinib (LP-168) can bind wild-type BTK covalently and C481-mutated BTK non-covalently (reversibly).
Rocbrutinib (LP-168) reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration, shows preclinical activity in resistant CLL models.

Physicochemical Properties

M.Wt 761.93
Formula C42H51N9O5
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

N-[5-[[6-[2-(1,3,4,6,7,8-Hexahydro-7,7-dimethyl-1-oxo-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-2-yl)-3-(hydroxymethyl)-4-pyridinyl]-3,4-dihydro-4-methyl-3-oxo-2-pyrazinyl]amino]-2-[(2S)-2-methyl-4-(tetrahydro-2H-pyran-4-yl)-1-piperazinyl]phenyl]-2-propenamide

References

1. Patent WO2020176403 A1.
2. Britten Gordon BS, et al. Blood (2025) 146 (Supplement 1): 1532.

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