A selective BMX and BTK inhibitor
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BMX-IN-1

Item No. 19165

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-methyl-5-[9-[4-[(methylsulfonyl)amino]phenyl]-2-oxobenzo[h]-1,6-naphthyridin-1(2H)-yl]phenyl]-2-propenamide
CAS Number
1431525-23-3
Synonyms
  • BMX Inhibitor 1
Molecular Formula
C29H24N4O4S
Formula Weight
524.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mLDMSO: 30 mg/mLDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL
λmax
260, 298 nm
SMILES
CS(NC1=CC=C(C2=CC=C(N=CC(C=C3)=C4N(C5=CC(NC(C=C)=O)=C(C)C=C5)C3=O)C4=C2)C=C1)(=O)=O
InChi Code
InChI=1S/C29H24N4O4S/c1-4-27(34)31-26-16-23(12-5-18(26)2)33-28(35)14-9-21-17-30-25-13-8-20(15-24(25)29(21)33)19-6-10-22(11-7-19)32-38(3,36)37/h4-17,32H,1H2,2-3H3,(H,31,34)
InChi Key
SFMJNHNUOVADRW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    Product Description

    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX; IC50 = 8 nM) that targets Cys496 in the BMX ATP binding domain.1 It additionally targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent for inhibition of Blk, JAK3, EGFR, Itk, or Tec activity. BMX-IN-1 was shown to inhibit the proliferation of Tel-BMX-transformed Ba/F3 prostate cancer cells with a GI50 value of 25 nM.1 Antiproliferative activity was also observed in RV-1, DU-145, PC-3, and VCAP prostate cancer cell lines (GI50s = 2.54, 4.38, 5.37, and 2.46 µM, respectively).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, F., Zhang, X., Weisberg, E., et al. Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem. Biol. 8(7), 1423-1428 (2013).