A DNA polymerase θ inhibitor
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ART812

Item No. 42904

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,3S,4S)-N-(3-chloro-4-fluorophenyl)-3,4-dihydroxy-N-methyl-1-[6-methyl-4-(trifluoromethyl)-2-pyridinyl]-5-oxo-2-pyrrolidinecarboxamide
CAS Number
2607138-82-7
Molecular Formula
C19H16ClF4N3O4
Formula Weight
461.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C1N(C2=CC(C(F)(F)F)=CC(C)=N2)[C@H](C(N(C)C3=CC=C(F)C(Cl)=C3)=O)[C@H](O)[C@@H]1O
InChi Code
InChI=1S/C19H16ClF4N3O4/c1-8-5-9(19(22,23)24)6-13(25-8)27-14(15(28)16(29)18(27)31)17(30)26(2)10-3-4-12(21)11(20)7-10/h3-7,14-16,28-29H,1-2H3/t14-,15-,16-/m0/s1
InChi Key
YJJOABOMFPGRED-JYJNAYRXSA-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

    $87

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    5 mg

    $392

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    10 mg

    $609

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    25 mg

    $978

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    Cayman Chemical
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    Product Description

    ART812 is an inhibitor of DNA polymerase θ (IC50 = 7.6 nM).1 It inhibits microhomology-mediated end joining (MMEJ) in a reporter assay using HEK293 cells (EC50 = 240 nM). ART812 (150 mg/kg twice per day) increases blood levels of micronucleated reticulocytes in mice. It inhibits tumor development in a Brca1- and Shld2-knockout MDA-MB-436 breast cancer rat xenograft model of tumor initiation when administered at a dose of 100 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stockley, M.L., Benedetti, G., Blencowe, P., et al. Discovery, characterization, and structure-based optimization of small-molecule in vitro and in vivo probes for human DNA polymerase theta. J. Med. Chem. 65(20), 13879-13891 (2022).