PERK-IN-5
Based on 1 Customer Validation
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.
- Purity: 99.07%
- CAS No.: 2616821-91-9
- Formula: C25H26F2N4O3
- Molecular Weight:468.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 2 nM (PERK), 9 nM (p-eIF2α)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PERK-IN-5 (3 or 10 mg/kg; p.o.; twice daily, for 28 days) has statistically significant tumor growth inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 mice[1] (Pharmacokinetics)
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Dosage:3, 10, 30 and 100 mg/kg
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Administration:p.o.; 0.25-24 hours
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Result:Showed robust pharmacokinetics with Cmax of 3353 ng/mL, AUC0-last of 5153 h*ng/mL, and bioavailability of 70%.
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Animal Model:BALB/c nude female mice (inoculated subcutaneously with 786-O tumor cells)[1]
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Dosage:3 or 10 mg/kg
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Administration:p.o.; twice daily, for 28 days
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Result:Showed statistically significant tumor growth inhibition.
Chemical Information
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CAS No. 2616821-91-9
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Appearance Solid
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Molecular Weight 468.50
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Formula C25H26F2N4O3
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Color Off-white to light yellow
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SMILES
CCC1=C(C2=CN=C(N)C(C(NC(C)C)=O)=C2)C=CC(NC([C@@H](C3=CC(F)=CC(F)=C3)O)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 250 mg/mL (533.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1345 mL | 10.6724 mL | 21.3447 mL | 53.3618 mL |
| 5 mM | 0.4269 mL | 2.1345 mL | 4.2689 mL | 10.6724 mL | |
| 10 mM | 0.2134 mL | 1.0672 mL | 2.1345 mL | 5.3362 mL | |
| 15 mM | 0.1423 mL | 0.7115 mL | 1.4230 mL | 3.5575 mL | |
| 20 mM | 0.1067 mL | 0.5336 mL | 1.0672 mL | 2.6681 mL | |
| 25 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1345 mL | |
| 30 mM | 0.0711 mL | 0.3557 mL | 0.7115 mL | 1.7787 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3340 mL | |
| 50 mM | 0.0427 mL | 0.2134 mL | 0.4269 mL | 1.0672 mL | |
| 60 mM | 0.0356 mL | 0.1779 mL | 0.3557 mL | 0.8894 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5336 mL |
PERK-IN-5 Related Classifications
HY-145835 Related Classifications
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