An inhibitor of sortilin
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AF38469

Item No. 35530

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[(6-methyl-2-pyridinyl)amino]carbonyl]-5-(trifluoromethyl)-benzoic acid
CAS Number
1531634-31-7
Molecular Formula
C15H11F3N2O3
Formula Weight
324.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleEthanol: Soluble
λmax
283 nm
SMILES
O=C(C1=C(C(NC2=CC=CC(C)=N2)=O)C=CC(C(F)(F)F)=C1)O
InChi Code
InChI=1S/C15H11F3N2O3/c1-8-3-2-4-12(19-8)20-13(21)10-6-5-9(15(16,17)18)7-11(10)14(22)23/h2-7H,1H3,(H,22,23)(H,19,20,21)
InChi Key
JWCUSQCZMQIBMR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $74

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    5 mg

    $329

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    10 mg

    $585

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    25 mg

    $1,094

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    Cayman Chemical
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    Product Description

    AF38469 is an inhibitor of sortilin, also known as the neurotensin-3 receptor (NTS3; IC50 = 330 nM).1 It is selective for sortilin over neurotensin-1 (NTS1), δ-opioid, angiotensin II type 1 (AT1), endothelin A (ETA), and ETB receptors, GPR40, PPARδ, and matrix metalloproteinase-12 (MMP-12), and the prostaglandin E2 (PGE2) receptor subtype EP1. AF38469 (400 nM) inhibits the epithelial-to-mesenchymal transition (EMT) in, and reduces migration and invasion of, U87 and A172 glioblastoma cells.2 It also reduces tumor growth in a glioblastoma multiforme mouse xenograft model when administered at a dose of 0.01 g/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schrøder, T.J., Christensen, S., Lindberg, S., et al. The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorg. Med. Chem. Lett. 24(1), 177-180 (2014).

    2. Yang, W., Wu, P.-F., Ma, J.-X., et al. Sortilin promotes glioblastoma invasion and mesenchymal transition through GSK-3β/β-catenin/twist pathway. Cell Death Dis. 10(3), 208 (2019).