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BAY-8400

Chemical Structure : BAY-8400

CAS No.: 2763602-59-9

BAY-8400 (BAY8400)

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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5 mg $258 In stock
10 mg $398 In stock
25 mg $598 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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,

Physicochemical Properties

M.Wt 393.398
Formula C21H17F2N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[1,2,4]Triazolo[4,3-a]quinoxaline, 8-[5-(difluoromethyl)-3-pyridinyl]-1-(2,3,6,7-tetrahydro-4-oxepinyl)-

References

1. Markus Berger, et al. J Med Chem. 2021 Sep 9;64(17):12723-12737.

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