AMG PERK 44 free base

AMG PERK 44 is an orally active and highly selective PERK inhibitor.

For research use only. Not for human or veterinary use.

Target PERK Autophagy

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AMG PERK 44 structure

CAS No.: 1883548-84-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02173-100mg	In stock	Get quote
250 mg	USD 950.00	BP-02173-250mg	In stock	Get quote
500 mg	USD 1,520.00	BP-02173-500mg	In stock	Get quote
1 g	USD 2,400.00	BP-02173-1g	In stock	Get quote
2 g	USD 3,800.00	BP-02173-2g	In stock	Get quote

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Description

AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy[1][2].

Biological activity

In Vitro AMG PERK 44 has an IC50 of 84 nM for cell pPERK. In Vivo AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation in this assay (ED50=3 mg/kg; ED90=60 mg/kg at the 4 hours time point), and >50% target coverage is maintained for 24 h in a time course PD assay when dosed at 100 mg/kg po. AMG PERK 44 (iv; 1 mg/kg) has a CL of 1.6 L/h kg, a Vss of 3.6 L/kg and MRT of 2.3 hours in Sprague-Dawley rats and male CD-1 mice.

Identifiers

SMILES: CC1=C(C(=C(C=C1)C(=O)C2=C(N(N(C2=O)C3=CC=CC=C3)C)C4=CC=CC=C4)N)C5=CC6=C(C=C5)N=C(C=C6)C.Cl
InChIKey: RNAKBTDDCHJCMT-UHFFFAOYSA-N

Specifications

MW (average): 561.0730
Formula: C₃₄H₂₉ClN₄O₂
CAS No.: 1883548-84-2
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, sealed storage, away from moisture; In solvent -20°C, 6 months;

Solubility

soluble in DMSO

Documents

References

[1]. Smith AL, et al. Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem. 2015 Feb 12;58(3):1426-41.

[2]. Roest G, et al. The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells. 2018 Nov 30;7(12). pii: E239.

Same target

Search PERK

Same research area

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