PERK-IN-5

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.

Product information

CAS Number: 2616821-91-9

Molecular Weight: 468.50

Formula: C25H26F2N4O3

Smiles: CC(C)NC(=O)C1=CC(=CN=C1N)C1=CC=C(C=C1CC)NC(=O)[C@H](O)C1C=C(F)C=C(F)C=1

InChiKey: YNDQMKBAYRFBMW-JOCHJYFZSA-N

InChi: InChI=1S/C25H26F2N4O3/c1-4-14-9-19(31-25(34)22(32)15-7-17(26)11-18(27)8-15)5-6-20(14)16-10-21(23(28)29-12-16)24(33)30-13(2)3/h5-13,22,32H,4H2,1-3H3,(H2,28,29)(H,30,33)(H,31,34)/t22-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Calvo V, 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. 2021;43:128058.

Products are for research use only. Not for human use.