PERK-IN-5 - ≥99% , CAS No.2616821-91-9

CAS: 2616821-91-9 Cat. No.: P649188 Fórmula: C₂₅H₂₆F₂N₄O₃ Peso molecular: 468.50

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Visão geral

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor ( IC 50 s 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

In Vitro

PERK-IN-5 (compound 28) (10-48 µM) is relatively stable in both human and dog hepatocytes and is characterized with long half-lives. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PERK-IN-5 (3-100 mg/kg; p.o.; 0.25-24 hours) has robust pharmacokinetics in CD1 mice, with C max of 3353 ng/mL, AUC 0-last of 5153 h*ng/mL, and bioavailability of 70% . PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD1 mice (Pharmacokinetics) Dosage: 3, 10, 30 and 100 mg/kg Administration: p.o.; 0.25-24 hours Result: Showed robust pharmacokinetics with C max of 3353 ng/mL, AUC 0-last of 5153 h*ng/mL, and bioavailability of 70%. Animal Model: BALB/c nude female mice (inoculated subcutaneously with 786-O tumor cells) Dosage: 3 or 10 mg/kg Administration: p.o.; twice daily, for 28 days Result: Showed statistically significant tumor growth inhibition.

Form:Solid

IC50& Target:IC 50 : 2 nM (PERK), 9 nM (p-eIF2α)

Specifications

Especificações e pureza

≥99%

Mecanismos bioquímicos e fisiológicos

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor ( IC 50 s 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.

Condições de armazenamento de armazenamento

Store at -20°C

Enviado em

Ice chest + Ice pads

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Pureza

≥99%

Nomes e identificadores

• Peso molecular: 468.50

Propriedades químicas e físicas

• Solubilidade: DMSO : 250 mg/mL (533.62 mM; Need ultrasonic)

Perguntas frequentes

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2616821-91-9, the molecular formula is C25H26F2N4O3, and the molecular weight is 468.50 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.