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AG14361

Chemical Structure : AG14361

CAS No.: 328543-09-5

AG14361 (AG 14361;AG-14361)

Catalog No.: PC-42846Not For Human Use, Lab Use Only.

AG14361 is a potent, specific and competitive inhibitor of PARP-1 with Ki of 5.8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AG14361 is a potent, specific and competitive inhibitor of PARP-1 with Ki of 5.8 nM。
AG14361 shows potent amplification of the cytotoxic effects of temozolomide (TM) and topotecan (TP) against A549 cells, inhibits LoVo Cell Line with GI50 of 11.2 uM alone。
AG14361 increases the delay of LoVo xenograft growth induced by irinotecan, x-irradiation, or temozolomide by two- to threefold with nontoxicity, causes complete regression of SW620 xenograft tumors combined with temozolomide.

Physicochemical Properties

M.Wt 320.3883
Formula C19H20N4O
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

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-

References

1. Veuger SJ, et al. Cancer Res. 2003 Sep 15;63(18):6008-15.

2. Skalitzky DJ, et al. J Med Chem. 2003 Jan 16;46(2):210-3.

3. Curtin NJ, et al. Clin Cancer Res. 2004 Feb 1;10(3):881-9.

4. Smith LM, et al. Clin Cancer Res. 2005 Dec 1;11(23):8449-57.

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