A covalent BTK inhibitor
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AVL-292

Item No. 17993

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-2-propenamide
CAS Number
1202757-89-8
Synonyms
  • CC-292
  • Spebrutinib
Molecular Formula
C22H22FN5O3
Formula Weight
423.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:30): 0.03 mg/mlEthanol: 0.5 mg/ml
λmax
271 nm
SMILES
FC(C(NC1=CC(NC(C=C)=O)=CC=C1)=N2)=CN=C2NC3=CC=C(OCCOC)C=C3
InChi Code
InChI=1S/C22H22FN5O3/c1-3-20(29)25-16-5-4-6-17(13-16)26-21-19(23)14-24-22(28-21)27-15-7-9-18(10-8-15)31-12-11-30-2/h3-10,13-14H,1,11-12H2,2H3,(H,25,29)(H2,24,26,27,28)
InChi Key
KXBDTLQSDKGAEB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    AVL-292 is a covalent inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 5.9 nM).1 It is selective for BTK over a panel of 61 kinases when used at a concentration of 1 µM but does inhibit the additional Tec family kinases BMX, Itk, Tec, and TXK (IC50s = 0.7, 36, 6.2, and 8.9 nM, respectively). AVL-292 inhibits naïve human B cell proliferation (EC50 = 3 nM). It reduces joint damage, pannus formation, cartilage degradation, and bone erosion in a mouse model of rheumatioid arthritis induced by collagen when used at doses of 3, 10, and 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Evans, E.K., Tester, R., Aslanian, S., et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J. Pharmacol. Exp. Ther. 346(2), 219-228 (2013).