2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. PKI-166

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.

PKI-166 Chemical Structure

PKI-166 Chemical Structure

CAS No. : 187724-61-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 490 In-stock
50 mg USD 800 In-stock
100 mg USD 1280 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PKI-166:

PKI-166 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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]
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.

PKI-166 Related Antibodies

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.
Molecular Weight

330.38

Formula

C20H18N4O
CAS No.
Appearance

Solid

Color

Off-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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0268 mL 15.1341 mL 30.2682 mL
5 mM 0.6054 mL 3.0268 mL 6.0536 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.58%

COA (250 KB) HNMR (278 KB) LCMS (96 KB)

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 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
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PKI-166 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKI-166187724-61-4PKI166PKI 166EGFREpidermal growth factor receptorErbB-1HER1tyrosinekinase,EGFR-TKIpancreaticcancerInhibitorinhibitorinhibit

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