An inhibitor of BUB1 kinase
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BAY-1816032

Item No. 35095

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[3,5-difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]-ethanol
CAS Number
1891087-61-8
Molecular Formula
C27H24F2N6O4
Formula Weight
534.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMSO: 10 mg/mlEthanol: Slightly solublePBS (pH 7.2): 0.20 mg/ml
λmax
217, 257, 309 nm
SMILES
FC1=C(CN2N=C(C3=C2C=CC=C3)C4=NC(NC5=C(OC)C=NC=C5)=C(OC)C=N4)C(F)=CC(OCCO)=C1
InChi Code
InChI=1S/C27H24F2N6O4/c1-37-23-13-30-8-7-21(23)32-26-24(38-2)14-31-27(33-26)25-17-5-3-4-6-22(17)35(34-25)15-18-19(28)11-16(12-20(18)29)39-10-9-36/h3-8,11-14,36H,9-10,15H2,1-2H3,(H,30,31,32,33)
InChi Key
QVOGVAVHOLLLAZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $194

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    10 mg

    $267

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    25 mg

    $603

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    Product Description

    BAY-1816032 is an inhibitor of the mitotic checkpoint serine/threonine protein kinase BUB1 (IC50 = 6.1 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Siemeister, G., Mengel, A., Fernández-Montalván, A.E., et al. Inhibition of BUB1 kinase by BAY 1816032 sensitizes tumor cells toward taxanes, ATR, and PARP inhibitors in vitro and in vivo. Clin. Cancer Res. 25(4), 1404-1414 (2019).