A DNA-PK inhibitor
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BAY-8400

Item No. 43707

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[5-(difluoromethyl)-3-pyridinyl]-1-(2,3,6,7-tetrahydro-4-oxepinyl)-[1,2,4]triazolo[4,3-a]quinoxaline
CAS Number
2763602-59-9
Molecular Formula
C21H17F2N5O
Formula Weight
393.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
FC(F)C1=CN=CC(C2=CC3=C(C=C2)N=CC4=NN=C(C5=CCCOCC5)N34)=C1
InChi Code
InChI=1S/C21H17F2N5O/c22-20(23)16-8-15(10-24-11-16)14-3-4-17-18(9-14)28-19(12-25-17)26-27-21(28)13-2-1-6-29-7-5-13/h2-4,8-12,20H,1,5-7H2
InChi Key
ATKHYZXUMVNCIO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $83

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    5 mg

    $330

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    10 mg

    $495

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    25 mg

    $1,032

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    Product Description

    BAY-8400 is an inhibitor of DNA-dependent protein kinase (DNA-PK; IC50 = 0.081 µM).1 It is selective for DNA-PK over ataxia-telangiectasia mutated kinase (ATM) and mTOR (IC50s = 19.3 and 1.91 µM, respectively) and a panel of 365 additional kinases at 1 µM but does inhibit ataxia-telangiectasia and Rad3-related protein/kinase (ATR) and PI3Kβ (IC50s = 0.394 and 0.117 µM, respectively). BAY-8400 inhibits the formation of γH2AX in ATM-negative HT-144 melanoma cells (IC50 = 0.069 nM) and reduces the proliferation of HT-29 colon cancer cells when used alone or in combination with bleomycin. In vivo, BAY-8400 (150 mg/kg, p.o.) reduces tumor area in an LNCaP prostate cancer mouse xenograft model when administered in combination with BAY 2315497.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Berger, M., Wortmann, L., Buchgraber, P., et al. BAY-8400: A novel potent and selective DNA-PK inhibitor which shows synergistic efficacy in combination with targeted alpha therapies. J. Med. Chem. 64(17), 12723-12737 (2021).