Cat. No.: HY-117155

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PKI-166

1 Cited Publications

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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

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PKI-166 Chemical Structure

CAS No.: 187724-61-4

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC₅₀ of 0.7 nM^[1].

IC₅₀ & Target

IC50: 0.7 nM (EGFR tyrosine kinase)^[1]

All EGFR Isoforms :

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.

Western Blot Analysis^[1]

Cell Line:

L3.6pl cells
Concentration:

0.01 μM, 0.05 μM, 0.5 μM
Incubation Time:

1 hour
Result:

Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay^[1]

Cell Line:

L3.6pl cells
Concentration:

0.03 μM
Incubation Time:

6 days
Result:

Enhanced the cytotoxicity mediated by gemcitabine.

In Vivo

PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth^[1].

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

Animal Model:

Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)^[1]
Dosage:

100 mg/kg
Administration:

Oral administration; daily; from day 7 to day 35 after xenograft
Result:

Significantly decreased median tumor volume.

Chemical Information

CAS No. 187724-61-4
Appearance Solid
Molecular Weight 330.38
Formula C₂₀H₁₈N₄O
Color White to light yellow
SMILES

OC1=CC=C(C2=CC3=C(N=CN=C3N2)N[C@@H](C4=CC=CC=C4)C)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0268 mL

15.1341 mL

30.2682 mL

5 mM

0.6054 mL

3.0268 mL

6.0536 mL

10 mM

0.3027 mL

1.5134 mL

3.0268 mL

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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	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

Keywords

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PKI-166

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PKI-166

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PKI-166

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PKI-166

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PKI-166 Related Classifications

HY-117155 Related Classifications