A BTK inhibitor
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Pirtobrutinib

Item No. 36775

Technical Information
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
Purity
≥98%
A solid
DMF: 3 mg/mlDMSO: 5 mg/mlEthanol: 5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Pirtobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK).1 It inhibits wild-type and mutant BTK (IC50s = 10-100 and <10 nM for wild-type BTK and BTKC481S, 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Guisot, N. Compounds useful as kinase inhibitors. (2017).

    2. Aslan, B., Kismali, G., Iles, L.R., et alPirtobrutinib inhibits wild-type and mutant Bruton’s tyrosine kinase-mediated signaling in chronic lymphocytic leukemia. Blood Cancer J. 12(5), 80 (2022).