Pirtobrutinib

Pirtobrutinib is an inhibitor of Bruton's tyrosine kinase (BTK). It inhibits wild-type and mutant BTK (IC50s = 10-100 and C481S, respectively). It is selective for BTK over EGFR (IC50 = 1-10 µM). Pirtobrutinib decreases the number of Ki67-positive cells, a marker of cell proliferation, in MEC-1 chronic lymphocytic leukemia (CLL) mouse xenograft models using MEC-1 cells that express either wild-type BTK or BTKC481S.Formal Name: 5-amino-3-[4-[[(5-fluoro-2-methoxybenzoyl)amino]methyl]phenyl]-1-[(1S)-2,2,2-trifluoro-1-methylethyl]-1H-pyrazole-4-carboxamide. CAS Number: 2101700-15-4. Synonyms: LOXO-305, LY3527727. Molecular Formula: C22H21F4N5O3. Formula Weight: 479.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, Ethanol: 5 mg/ml, PBS (pH 7.2): insol. lambdamax: 234 nm. SMILES: O=C(C1=C(C=CC(F)=C1)OC)NCC(C=C2)=CC=C2C3=NN([C@H](C(F)(F)F)C)C(N)=C3C(N)=O. InChi Code: InChI=1S/C22H21F4N5O3/c1-11(22(24,25)26)31-19(27)17(20(28)32)18(30-31)13-5-3-12(4-6-13)10-29-21(33)15-9-14(23)7-8-16(15)34-2/h3-9,11H,10,27H2,1-2H3,(H2,28,32)(H,29,33)/t11-/m0/s1. InChi Key: FWZAWAUZXYCBKZ-NSHDSACASA-N.