1. Cell Cycle/DNA Damage
  2. PERK
  3. PERK-IN-5

PERK-IN-5 

Cat. No.: HY-145835
Handling Instructions

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.

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

PERK-IN-5 Chemical Structure

PERK-IN-5 Chemical Structure

CAS No. : 2616821-91-9

Size Price Stock
5 mg USD 750 Ask For Quote & Lead Time
10 mg USD 1200 Ask For Quote & Lead Time
25 mg USD 2400 Ask For Quote & Lead Time
50 mg USD 3900 Ask For Quote & Lead Time
100 mg USD 6300 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

IC50: 2 nM (PERK), 9 nM (p-eIF2α)[1]

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[1].

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 Cmax of 3353 ng/mL, AUC0-last of 5153 h*ng/mL, and bioavailability of 70%[1].
PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD1 mice[1] (Pharmacokinetics)
Dosage: 3, 10, 30 and 100 mg/kg
Administration: p.o.; 0.25-24 hours
Result: Showed robust pharmacokinetics with Cmax of 3353 ng/mL, AUC0-last of 5153 h*ng/mL, and bioavailability of 70%.
Animal Model: BALB/c nude female mice (inoculated subcutaneously with 786-O tumor cells)[1]
Dosage: 3 or 10 mg/kg
Administration: p.o.; twice daily, for 28 days
Result: Showed statistically significant tumor growth inhibition.
Molecular Weight

468.50

Formula

C25H26F2N4O3

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PERK-IN-5
Cat. No.:
HY-145835
Quantity:
MCE Japan Authorized Agent: