An irreversible inhibitor of BMX (IC50 = 8 nM) and BTK (IC50 = 10.4 nM); inhibits the proliferation of Tel-BMX-transformed Ba/F3 prostate cancer cells (GI50 = 25 nM)

BMX-IN-1 – 500 µg

Brand:
Cayman
CAS:
1431525-23-3
Storage:
-20
UN-No:
Non-Hazardous - /

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.{31496} 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.{31496} 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).{31496}  

 

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Description

An irreversible inhibitor of BMX (IC50 = 8 nM) and BTK (IC50 = 10.4 nM); inhibits the proliferation of Tel-BMX-transformed Ba/F3 prostate cancer cells (GI50 = 25 nM), as well as RV-1, DU-145, PC-3, and VCAP prostate cancer cell lines (GI50s = 2.54, 4.38, 5.37, and 2.46 µM, respectively)

Formal name: N-[2-methyl-5-[9-[4-[(methylsulfonyl)amino]phenyl]-2-oxobenzo[h]-1,6-naphthyridin-1(2H)-yl]phenyl]-2-propenamide

Synonyms:  BMX Inhibitor 1

Molecular weight: 524.6

CAS: 1431525-23-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Tec Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Tec Family Signaling

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