A PARP1 inhibitor
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AG-14361

Item No. 24677

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one
CAS Number
328543-09-5
Molecular Formula
C19H20N4O
Formula Weight
320.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 0.1 mg/ml
λmax
210, 240, 312 nm
SMILES
O=C1NCCN2C3=C1C=CC=C3N=C2C4=CC=C(CN(C)C)C=C4
InChi Code
InChI=1S/C19H20N4O/c1-22(2)12-13-6-8-14(9-7-13)18-21-16-5-3-4-15-17(16)23(18)11-10-20-19(15)24/h3-9H,10-12H2,1-2H3,(H,20,24)
InChi Key
SEKJSSBJKFLZIT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    AG-14361 is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; Ki = 6.3 nM for the human enzyme).1 It inhibits PARP1 activity in permeabilized and intact SW620 cells (IC50s = 29 and 14 nM, respectively).2 AG-14361 (0.4 µM) potentiates the growth inhibitory effects of temozolomide (Item No. 14163) in HCT116, A2480, and CP70 cells and of the topoisomerase I inhibitor topotecan (Item No. 14129) by greater than three-fold in PARP1+/+ primary embryonic fibroblasts.3,4 It slows the rejoining of camptothecin-induced DNA strand breaks.4 AG-14361 also inhibits cell growth in a PARP1-independent manner with GI50 values of 66 and 65 µM, respectively, in cell lines derived from PARP1+/+ and PARP1-/- mice.2 AG-14361 (15 mg/kg), in combination with temozolomide, leads to tumor regression in an SW620 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Skalitzky, D.J., Marakovits, J.T., Maegley, K.A., et al. Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J. Med. Chem. 46(2), 210-213 (2003).

    2. Calabrese, C.R., Almassy, R., Barton, S., et al. Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361. J. Natl. Cancer Inst. 96(1), 56-67 (2004).

    3. Curtin, N.J., Wang, L.Z., Yiakouvaki, A., et al. Novel poly(ADP-ribose) polymerase-1 inhibitor, AG14361, restores sensitivity to temozolomide in mismatch repair-deficient cells. Clin. Cancer Res. 10(3), 881-889 (2004).

    4. Smith, L.M., Willmore, E., Austin, C.A., et al. The novel poly(ADP-Ribose) polymerase inhibitor, AG14361, sensitizes cells to topoisomerase I poisons by increasing the persistence of DNA strand breaks. Clin. Cancer Res. 11(23), 8449-8457 (2005).