Cat. No.: HY-13896

PD168393

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC₅₀=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.

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Pureté: 98.01%
CAS No.: 194423-15-9
Formule: C₁₇H₁₃BrN₄O
Masse moléculaire:369.22

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PD168393 Chemical Structure

CAS No.: 194423-15-9

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

EGFR

0.7 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	4.3 nM Compound: 5a	Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor (EGFR) in A431 cells Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor (EGFR) in A431 cells	[PMID: 10346932]
A-431	IC₅₀	2.7 nM Compound: 3	Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting	[PMID: 10753475]
A-431	IC₅₀	2.7 nM Compound: 4	Inhibition of autophosphorylation of EGFR in A431 cells Inhibition of autophosphorylation of EGFR in A431 cells	[PMID: 11462982]
A-431	IC₅₀	0.095 μM Compound: 2	Inhibition of human epidermoid carcinoma xenograft (A431) tumor growth Inhibition of human epidermoid carcinoma xenograft (A431) tumor growth	[PMID: 11495584]
A-431	IC₅₀	1.96 μM Compound: 3, PD-168393	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	[PMID: 17154492]
A-431	IC₅₀	0.012 μM Compound: 2, PD-168393	Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot	[PMID: 20151670]
A-431	IC₅₀	0.152 μM Compound: 2, PD-168393	Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot	[PMID: 20151670]
A-431	IC₅₀	0.036 μM Compound: PD168393	Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA	[PMID: 27135370]
A-431	IC₅₀	1.96 μM Compound: PD168393	Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 27135370]
A549	IC₅₀	17.9 nM Compound: 2, PD168393	Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis	[PMID: 23988354]
A549	IC₅₀	3.94 nM Compound: 2, PD168393	Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis	[PMID: 23988354]
BaF3	IC₅₀	>10 μM Compound: PD-168393	Inhibition of Blk expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of Blk expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	>10 μM Compound: PD-168393	Inhibition of JAK3 expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of JAK3 expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	0.303 μM Compound: PD-168393	Inhibition of Bmx expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of Bmx expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	0.324 μM Compound: PD-168393	Inhibition of wild type Bmx expressed in mouse BAF3 cells assessed as cytotoxicity Inhibition of wild type Bmx expressed in mouse BAF3 cells assessed as cytotoxicity	[PMID: 18667312]
BaF3	IC₅₀	8.58 /μM/s Compound: PD-168393	Inhibition of Bmx C496S mutant expressed in mouse BAF3 cells Inhibition of Bmx C496S mutant expressed in mouse BAF3 cells	[PMID: 18667312]
BaF3	IC₅₀	8.58 μM Compound: PD-168393	Inhibition of Bmx C496S mutant expressed in mouse BAF3 cells Inhibition of Bmx C496S mutant expressed in mouse BAF3 cells	[PMID: 18667312]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	<0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
BaF3	GI₅₀	>0.5 μM Compound: 3b	Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay	[PMID: 20222733]
MDA-MB-453	IC₅₀	5.7 nM Compound: 5a	Inhibition of heregulin-stimulated autophosphorylation of ERBB2 receptor kinase in MDA-MB-453 cells. Inhibition of heregulin-stimulated autophosphorylation of ERBB2 receptor kinase in MDA-MB-453 cells.	[PMID: 10346932]
NCI-H1975	IC₅₀	0.61 μM Compound: 2, PD-168393	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 20151670]
NCI-H1975	IC₅₀	0.028 μM Compound: I	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as inhibition of EGF-mediated autophosphorylation incubated for 30 mins prior to EGF challenge by cytoblot assay Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as inhibition of EGF-mediated autophosphorylation incubated for 30 mins prior to EGF challenge by cytoblot assay	10.1039/C3MD00118K
NCI-H1975	IC₅₀	0.44 μM Compound: I	Cytotoxicity against gefitinib-resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay Cytotoxicity against gefitinib-resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay	10.1039/C3MD00118K
Sf9	IC₅₀	<0.001 μM Compound: 2, PD-168393	Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay	[PMID: 17334377]
SK-BR-3	IC₅₀	0.015 μM Compound: 2	Inhibition of cell growth of SKBr3 cell lines using cell-based assay Inhibition of cell growth of SKBr3 cell lines using cell-based assay	[PMID: 11495584]
SK-BR-3	IC₅₀	0.2 μM Compound: I	Cytotoxicity against human SKBR3 cells expressing wild type EGFR assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay Cytotoxicity against human SKBR3 cells expressing wild type EGFR assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay	10.1039/C3MD00118K
SW-620	IC₅₀	4.133 μM Compound: 2	Inhibition of cell growth of SW620 cell lines using cell-based assay Inhibition of cell growth of SW620 cell lines using cell-based assay	[PMID: 11495584]
SW-620	IC₅₀	8.23 μM Compound: 2, PD-168393	Cytotoxicity against human SW620 cells after 72 hrs by MTT assay Cytotoxicity against human SW620 cells after 72 hrs by MTT assay	[PMID: 20151670]

In Vitro

PD168393 inhibits ligand-dependent receptor phosphorylation and inhibits EGF-induced tyrosine phosphorylation in A431 cells and Heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC₅₀ values of 4.3 nM and 5.7 nM, respectively^[1].

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

In Vivo

PD168393 (intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28) is effective in vivo, and produces tumor growth inhibition of 115% after 15 days’ treatment in human epidermoid carcinoma xenografts in mice^[1].

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

Animal Model:

A431 human epidermoid carcinoma grown as a xenograft in nude mice^[1]
Dosage:

58 mg/kg
Administration:

Intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28
Result:

Suppressed the growth of human epidermoid carcinoma xenografts.

Chemical Information

CAS No. 194423-15-9
Appearance Solid
Masse moléculaire 369.22
Formule C₁₇H₁₃BrN₄O
Color Light yellow to khaki
SMILES

C=CC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Cell Death Dis

RNAi-based ALOX15B silencing augments keratinocyte inflammation in vitro via EGFR/STAT1/JAK1 signalling. [Abstract]

2025 Jan 22;16(1):39. PMID: 39843435
J Cell Biochem

Epiregulin (EREG) is upregulated through an IL-1β autocrine loop in Caco-2 epithelial cells with reduced CFTR function. [Abstract]

2018 Mar;119(3):2911-2922. PMID: 29091309
Biochem Cell Biol

Epidermal growth factor receptor activity upregulates lactate dehydrogenase A expression, lactate dehydrogenase activity, and lactate secretion in cultured IB3-1 cystic fibrosis lung epithelial cells. [Abstract]

2021 Aug;99(4):476-487. PMID: 33481676

Solvant et solubilité

In Vitro:

DMSO : ≥ 30 mg/mL (81.25 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

2.7084 mL

13.5421 mL

27.0841 mL

5 mM

0.5417 mL

2.7084 mL

5.4168 mL

10 mM

0.2708 mL

1.3542 mL

2.7084 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 3.33 mg/mL (9.02 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (392 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[1]. D W Fry, et al. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7084 mL	13.5421 mL	27.0841 mL	67.7103 mL
	5 mM	0.5417 mL	2.7084 mL	5.4168 mL	13.5421 mL
	10 mM	0.2708 mL	1.3542 mL	2.7084 mL	6.7710 mL
	15 mM	0.1806 mL	0.9028 mL	1.8056 mL	4.5140 mL
	20 mM	0.1354 mL	0.6771 mL	1.3542 mL	3.3855 mL
	25 mM	0.1083 mL	0.5417 mL	1.0834 mL	2.7084 mL
	30 mM	0.0903 mL	0.4514 mL	0.9028 mL	2.2570 mL
	40 mM	0.0677 mL	0.3386 mL	0.6771 mL	1.6928 mL
	50 mM	0.0542 mL	0.2708 mL	0.5417 mL	1.3542 mL
	60 mM	0.0451 mL	0.2257 mL	0.4514 mL	1.1285 mL
	80 mM	0.0339 mL	0.1693 mL	0.3386 mL	0.8464 mL

Keywords

PD168393

3 Cited Publications

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PD168393

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Publications Citing Use of MedChemExpress (MCE) PD168393

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PD168393 Related Classifications

HY-13896 Related Classifications