A PERK inhibitor
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HC-5404

Item No. 45588

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-amino-5-[4-[[(2R)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]amino]-2-methylphenyl]-N-(1-methylethyl)-3-pyridinecarboxamide
CAS Number
2247396-91-2
Synonyms
  • LY-4
Molecular Formula
C24H24F2N4O3
Formula Weight
454.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Sparingly soluble: 1-10 mg/ml
SMILES
O=C(NC1=CC(C)=C(C2=CN=C(C(C(NC(C)C)=O)=C2)N)C=C1)[C@H](O)C3=CC(F)=CC(F)=C3
InChi Code
InChI=1S/C24H24F2N4O3/c1-12(2)29-23(32)20-9-15(11-28-22(20)27)19-5-4-18(6-13(19)3)30-24(33)21(31)14-7-16(25)10-17(26)8-14/h4-12,21,31H,1-3H3,(H2,27,28)(H,29,32)(H,30,33)/t21-/m1/s1
InChi Key
BRIWRAFDHZTJPE-OAQYLSRUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

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    Product Description

    HC-5404 is an inhibitor of protein kinase R-like ER kinase (PERK; IC50 = 4 nM in a cell-free assay).1 It is selective for PERK over a panel of 25 kinases at 1 mM. HC-5404 reduces the levels of phosphorylated eukaryotic translation initiation factor 2α subunit (eIF2α) in HEK293 cells (IC50 = 33 nM). It reduces tumor volume in a 786-O renal cell carcinoma mouse xenograft model when administered at a dose of 30 mg/kg once or twice per day.2 HC-5404 has an additive effect on tumor growth inhibition when administered in combination with axitinib (Item No. 13813), cabozantinib (XL184; Item No. 18464), lenvatinib (Item No. 19375), or sunitinib (Item No. 13159) in a 786-O mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Calvo, V., Surguladze, D., Li, A.H., et al. Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors. Bioorg. Med. Chem. Lett. 43, 128058 (2021).

    2. Stokes, M.E., Calvo, V., Fujisawa, S., et al. PERK inhibition by HC-5404 sensitizes renal cell carcinoma tumor models to antiangiogenic tyrosine kinase inhibitors. Clin. Cancer Res. 29(23), 4870-4882 (2023).