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Datasheet of NU-7441

Description:
KU-57788(NU7441) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 value of are 14
nM; 1700, 5000, >100000 and >100000 nM for mTOR, PI 3K, ATM and ATR respectively; also is a modest inhibitor of BRD4
and BRDT with IC50s of 1 and 3.5 uM respectively.
in vitro: NU7441 increased the cytotoxicity of ionizing radiation and etoposide in SW620, LoVo, and V3-YAC cells but not in
V3 cells, confirming that potentiation was due to DNA-PK inhibition. NU7441 substantially retarded the repair of ionizing
radiation-induced and etoposide-induced DSB. NU7441 appreciably increased G(2)-M accumulation induced by ionizing
radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 strongly inhibited DNA-PK in cell lines (IC(50) =
0.3 M) but only weakly inhibited PI3 K (IC(50) = 7 M). NU7441 caused doxorubicin- and IR-induced DNA DSBs (measured
by -H2AX foci) to persist and also slightly decreased homologous recombination activity, as assessed by Rad51 foci. NU7441 is
a modest inhibitor of BRD4 and BRDT (IC50 = 1 and 3.5 SM, respectively), which establishes a single hydrogen bond in the
KAc site through the chromenone oxygen with Asn140.
in vivo: In mice bearing SW620 xenografts, NU7441 concentrations in the tumor necessary for chemopotentiation in vitro were
maintained for at least 4 hours at nontoxic doses. NU7441 increased etoposide-induced tumor growth delay 2-fold without
exacerbating etoposide toxicity to unacceptable levels.

Chemical Information
Catalog

DC3100

Purity of current batch:

>98%

Molecular Weight (MW)

413.49

Molecular Formula

C25H19NO3S

CAS No.

503468-95-9

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.