BAY-1816032

BAY-1816032

CAT N°: 35095
Price:

From 66.00 56.10

BAY-1816032 is an inhibitor of the mitotic checkpoint serine/threonine protein kinase BUB1 (IC50 = 6.1 nM).{62656} It is selective for BUB1 over FLT3 (IC50 = 4.2 µM) and 15 other kinases (IC50s = >10 µM for all). BAY-1816032 inhibits proliferation of a variety of cancer cells (median IC50 = 1.4 µM) and acts synergistically with the mitotic inhibitor paclitaxel (Item No. 10461) to increase the rate of chromosomal segregation defects during mitosis in HeLa cells. It reduces tumor growth in a SUM149 mouse xenograft model when administered at a dose of 25 mg/kg and has an additive effect on reducing tumor growth when used in combination with paclitaxel in the same model.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-[3,5-difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]-ethanol
  • Correlated keywords
    • BAY1816032 BUB-1 FLT-3 SUM149
  • Product Overview:
    BAY-1816032 is an inhibitor of the mitotic checkpoint serine/threonine protein kinase BUB1 (IC50 = 6.1 nM).{62656} It is selective for BUB1 over FLT3 (IC50 = 4.2 µM) and 15 other kinases (IC50s = >10 µM for all). BAY-1816032 inhibits proliferation of a variety of cancer cells (median IC50 = 1.4 µM) and acts synergistically with the mitotic inhibitor paclitaxel (Item No. 10461) to increase the rate of chromosomal segregation defects during mitosis in HeLa cells. It reduces tumor growth in a SUM149 mouse xenograft model when administered at a dose of 25 mg/kg and has an additive effect on reducing tumor growth when used in combination with paclitaxel in the same model.

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