A DNA methyltransferase inhibitor
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Isomer(s)
11165SGI-1027
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MC3343

Item No. 43331

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[(2-amino-6-methyl-4-pyrimidinyl)amino]phenyl]-3-(4-quinolinylamino)-benzamide
CAS Number
1535187-91-7
Molecular Formula
C27H23N7O
Formula Weight
461.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C1=CC(NC2=C3C=CC=CC3=NC=C2)=CC=C1)NC4=CC(NC5=NC(N)=NC(C)=C5)=CC=C4
InChi Code
InChI=1S/C27H23N7O/c1-17-14-25(34-27(28)30-17)32-20-8-5-9-21(16-20)33-26(35)18-6-4-7-19(15-18)31-24-12-13-29-23-11-3-2-10-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34)
InChi Key
GRGNBXUBKBUEDX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

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    Product Description

    MC3343 is a DNA methyltransferase (DNMT) inhibitor (IC50s = 9 and 2.8 µM for DNMT1 and the DNMT3A2/DNMT3L complex, respectively).1 It is selective for these DNMTs over protein arginine methyltransferase 1 (PRMT1) and G9a-like protein. MC3343 selectively decreases the viability of U937 and Raji lymphoma cells and PC3 prostate and MDA-MB-231 breast cancer cells over isolated peripheral blood mononuclear cells (PBMCs; IC50s = 4.3, 8.8, 6.6, 9.7, and 57.4 µM, respectively). In vivo, MC3343 (50 mg/kg) decreases tumor volume in a patient-derived xenograft (PDX) mouse model of osteosarcoma when used alone or in combination with doxorubicin (Item No. 15007).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Valente, S., Liu, Y., Schnekenburger, M., et al. Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J. Med. Chem. 57(3), 701-713 (2014).

    2. Manara, M.C., Valente, S., Cristalli, C., et al. A quinoline-based DNA methyltransferase inhibitor as a possible adjuvant in osteosarcoma therapy. Mol. Cancer Ther. 17(9), 1881-1892 (2018).