An inhibitor of topoisomerase I
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Genz-644282

Item No. 24193

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3-dimethoxy-12-[2-(methylamino)ethyl]-benzo[c][1,3]benzodioxolo[5,6-h][1,6]naphthyridin-13(12H)-one
CAS Number
529488-28-6
Molecular Formula
C22H21N3O5
Formula Weight
407.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.5 mg/mlDMSO: 0.5 mg/mlDMSO:PBS (pH 7.2) (1:20): 0.04 mg/mlEthanol: 0.2 mg/ml
λmax
288 nm
SMILES
COC1=CC(C(N2CCNC)=O)=C(C=C1OC)C3=C2C4=CC(OCO5)=C5C=C4N=C3
InChi Code
InChI=1S/C22H21N3O5/c1-23-4-5-25-21-14-8-19-20(30-11-29-19)9-16(14)24-10-15(21)12-6-17(27-2)18(28-3)7-13(12)22(25)26/h6-10,23H,4-5,11H2,1-3H3
InChi Key
BAORCAMWLWRZQG-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

    $387

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    25 mg

    $801

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    Product Description

    Genz-644282 is a topoisomerase I (TOP-I) inhibitor that inhibits TOP-I-mediated DNA cleavage 10-fold more potently than the TOP-I inhibitor topotecan (Item No. 14129).1 It inhibits the growth of and is cytotoxic to human and mouse bone marrow cells in a colony-forming unit assay (IC50s = 0.4 and 2.3 nM, respectively; IC90s = 1.2 and 8.4 nM, respectively).2 It also inhibits the growth of and is cytotoxic to human tumor cell lines (IC50s = 0.15-2 nM; IC90s = 0.7-8.3 nM). Genz-644282 inhibits tumor growth in mouse xenograft models when administered at doses ranging from 1.36 to 2.7 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ruchelman, A.L., Houghton, P.J., Zhou, N., et al. 5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: Variation of N-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance. J. Med. Chem. 48(3), 792-804 (2005).

    2. Kurtzberg, L.S., Roth, S., Krumbholz, R., et al. Genz-644282, a novel non-camptothecin topoisomerase I inhibitor for cancer treatment. Clin. Cancer Res. 17(9), 2777-2787 (2011).