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Chemical Structure : BAY-8400
Catalog No.: PC-72056Not For Human Use, Lab Use Only.
BAY-8400 (BAY8400) is a highly potent, selective inhibitor of DNA-PK with biochemical IC50 of 81 nM, cellular IC50 of 69 nM (γH2AX in HT-144).
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BAY-8400 (BAY8400) is a highly potent, selective inhibitor of DNA-PK with biochemical IC50 of 81 nM, cellular IC50 of 69 nM (γH2AX in HT-144).
BAY-8400 showed good selectivity against PI3K and ATR, ATM and mTOR. In the KINOMEscan panel, >50% inhibition activity of BAY-8400 at 1 uM was measured only for three out of 365 kinases, including DNA-PK.
BAY-8400 demonstrates very potent antiproliferative activity against HT-29 cells in combination with the radiomimetic bleomycin (IC50=358 nM), while its antiproliferative activity in monotherapy was sevenfold lower (IC50=2540 nM).
Combination of PSMA-targeted thorium-227 conjugate BAY 2315497 treatment of human prostate tumor-bearing mice with BAY-8400 oral treatment increased antitumor efficacy,
| M.Wt | 393.398 | |
| Formula | C21H17F2N5O | |
| Appearance | Solid | |
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1. Markus Berger, et al. J Med Chem. 2021 Sep 9;64(17):12723-12737.
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