PKI-166
Based on 1 publication(s) in Google Scholar
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
For research use only. We do not sell to patients.
- Purity: 98.92%
- CAS No.: 187724-61-4
- Formula: C20H18N4O
- Molecular Weight:330.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
Publications Citing Use of MedChemExpress (MCE) PKI-166
MoreAll EGFR Isoforms
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Biological Activity
Description
IC50 & Target
IC50: 0.7 nM (EGFR tyrosine kinase)[1]
In Vitro
Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L3.6pl cells
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Concentration:0.01 μM, 0.05 μM, 0.5 μM
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Incubation Time:1 hour
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Result:Inhibited EGFR autophosphorylation in a dose-dependent manner.
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Cell Line:L3.6pl cells
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Concentration:0.03 μM
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Incubation Time:6 days
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Result:Enhanced the cytotoxicity mediated by gemcitabine.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1]
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Dosage:100 mg/kg
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Administration:Oral administration; daily; from day 7 to day 35 after xenograft
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Result:Significantly decreased median tumor volume.
Chemical Information
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CAS No. 187724-61-4
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Appearance Solid
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Molecular Weight 330.38
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Formula C20H18N4O
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Color White to light yellow
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SMILES
OC1=CC=C(C2=CC3=C(N=CN=C3N2)N[C@@H](C4=CC=CC=C4)C)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618
Solvent & Solubility
In Vitro:
DMSO : ≥ 125 mg/mL (378.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0268 mL | 15.1341 mL | 30.2682 mL | 75.6704 mL |
| 5 mM | 0.6054 mL | 3.0268 mL | 6.0536 mL | 15.1341 mL | |
| 10 mM | 0.3027 mL | 1.5134 mL | 3.0268 mL | 7.5670 mL | |
| 15 mM | 0.2018 mL | 1.0089 mL | 2.0179 mL | 5.0447 mL | |
| 20 mM | 0.1513 mL | 0.7567 mL | 1.5134 mL | 3.7835 mL | |
| 25 mM | 0.1211 mL | 0.6054 mL | 1.2107 mL | 3.0268 mL | |
| 30 mM | 0.1009 mL | 0.5045 mL | 1.0089 mL | 2.5223 mL | |
| 40 mM | 0.0757 mL | 0.3784 mL | 0.7567 mL | 1.8918 mL | |
| 50 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5134 mL | |
| 60 mM | 0.0504 mL | 0.2522 mL | 0.5045 mL | 1.2612 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9459 mL | |
| 100 mM | 0.0303 mL | 0.1513 mL | 0.3027 mL | 0.7567 mL |
PKI-166 Related Classifications
HY-117155 Related Classifications
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