A DHODH inhibitor
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AG-636

Item No. 36122

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-methyl-5-(2′-methyl[1,1′-biphenyl]-4-yl)-1H-benzotriazole-7-carboxylic acid
CAS Number
1623416-31-8
Molecular Formula
C21H17N3O2
Formula Weight
343.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleWater: slightly soluble
λmax
259 nm
SMILES
O=C(C1=CC(C2=CC=C(C3=C(C)C=CC=C3)C=C2)=CC4=C1N(C)N=N4)O
InChi Code
InChI=1S/C21H17N3O2/c1-13-5-3-4-6-17(13)15-9-7-14(8-10-15)16-11-18(21(25)26)20-19(12-16)22-23-24(20)2/h3-12H,1-2H3,(H,25,26)
InChi Key
GSBZRCGZLMBSNY-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

    $62

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    5 mg

    $244

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    10 mg

    $425

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    25 mg

    $605

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    Cayman Chemical
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    Product Description

    AG-636 is a dihydroorotate dehydrogenase (DHODH) inhibitor (IC50 = 17 nM).1 It increases levels of ureidosuccinic acid (Item No. 34126) and DHO, pyrimidine biosynthesis metabolites upstream of DHODH, in a panel of six cell lines when used at a concentration of 1 µM. AG-636 (100 mg/kg) induces complete tumor stasis in an OCI-Ly19 diffuse large B cell lymphoma (DLBCL) mouse xenograft model and complete tumor regression in a Z-138 ibrutinib-resistant mantle cell lymphoma mouse xenograft model. It also increases DHO levels and reduces pyrimidine levels in Z-138 and JeKo-1 lymphoma mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McDonald, G., Chubukov, V., Coco, J., et al. Selective vulnerability to pyrimidine starvation in hematologic malignancies revealed by AG-636, a novel clinical-stage inhibitor of dihydroorotate dehydrogenase. Mol. Cancer Ther. 19(12), 2502-2515 (2020).