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  3. AMG PERK 44

AMG PERK 44 

Cat. No.: HY-12661A Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

AMG PERK 44 Chemical Structure

AMG PERK 44 Chemical Structure

CAS No. : 1883548-84-2

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10 mM * 1 mL in DMSO USD 1420 Get quote
1 mg USD 230 In-stock
Estimated Time of Arrival: December 31
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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[1][2].

IC50 & Target

IC50: 6 nM (PERK)[1]

In Vitro

AMG PERK 44 has an IC50 of 84 nM for cell pPERK[1].

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[1].
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[1].

Animal Model: Four- to six-week old naive athymic nude mice[1]
Dosage: 3, 10, 30, 100 mg/kg
Administration: Orally
Result: Robustly inhibited PERK autophosphorylation in this assay (ED50=3 mg/kg; ED90=60 mg/kg at the 4 hours time point).
Animal Model: Sprague-Dawley rats and male CD-1 mice[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: Iv
Result: Had a CL of 1.6 L/h•kg, a Vss of 3.6 L/kg and a MRT of 2.3 hours.
Molecular Weight

561.07

Formula

C₃₄H₂₉ClN₄O₂

CAS No.

1883548-84-2

SMILES

O=C1N(C2=CC=CC=C2)N(C)C(C3=CC=CC=C3)=C1C(C4=CC=C(C)C(C5=CC=C6N=C(C)C=CC6=C5)=C4N)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

AMG PERK 44AMG PERK44AMG PERK-44PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseorallyGCN2B-RafInhibitorinhibitorinhibit

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AMG PERK 44
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HY-12661A
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