PD168393

Name: PD168393
Brand: MedChemExpress
SKU: HY-13896
Rating: 5.0 (3 reviews)

Art. -Nr.: HY-13896 Reinheit: 98.01%: Data Sheet
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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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PD168393 Chemische Struktur

CAS. Nr. : 194423-15-9

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10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE PD168393

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle EGFR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

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

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Beschreibung

IC₅₀ & Target^[1]

EGFR

0.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	1.96 3 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 3 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	0.036 3 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	0.012 3 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	1.96 3 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]
A-431	IC₅₀	0.036 3 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	0.012 3 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 3 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	0.095 3 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 3 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]
A-431	IC₅₀	0.152 3 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	1.96 3 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	0.152 3 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 3 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	0.095 3 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	2.7 1 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	1.96 3 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	1.96 3 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]
BaF3	GI₅₀	>0.5 3 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]
A549	IC₅₀	17.9 1 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]
A-431	IC₅₀	2.7 1 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]
A549	IC₅₀	3.94 1 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	GI₅₀	<0.5 3 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 3 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	IC₅₀	>10 3 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]
A-431	IC₅₀	2.7 1 Compound: 4	Inhibition of autophosphorylation of EGFR in A431 cells Inhibition of autophosphorylation of EGFR in A431 cells	[PMID: 11462982]
A-431	IC₅₀	4.3 1 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]
BaF3	IC₅₀	8.58 95 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 3 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 3 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	IC₅₀	0.303 3 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	GI₅₀	< 0.5 3 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	IC₅₀	0.324 3 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	GI₅₀	< 0.5 3 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]
A-431	IC₅₀	2.7 1 Compound: 4	Inhibition of autophosphorylation of EGFR in A431 cells Inhibition of autophosphorylation of EGFR in A431 cells	[PMID: 11462982]
BaF3	GI₅₀	< 0.5 3 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]
A-431	IC₅₀	2.7 1 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]
BaF3	GI₅₀	< 0.5 3 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]
A549	IC₅₀	3.94 1 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	GI₅₀	> 0.5 3 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]
A-431	IC₅₀	4.3 1 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]
NCI-H1975	IC₅₀	0.028 3 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
MDA-MB-453	IC₅₀	5.7 1 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]
A549	IC₅₀	17.9 1 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]
NCI-H1975	IC₅₀	0.44 3 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
NCI-H1975	IC₅₀	0.61 3 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	0.61 3 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]
Sf9	IC₅₀	< 0.001 3 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]
NCI-H1975	IC₅₀	0.44 3 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
SK-BR-3	IC₅₀	0.015 3 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]
NCI-H1975	IC₅₀	0.028 3 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
Sf9	IC₅₀	<0.001 3 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	0.2 3 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 3 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]
SK-BR-3	IC₅₀	0.2 3 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
SK-BR-3	IC₅₀	0.015 3 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]
SW-620	IC₅₀	8.23 3 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]
SW-620	IC₅₀	8.23 3 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]
SW-620	IC₅₀	4.133 3 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]
A549	IC₅₀	17.9 1 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 1 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	GI₅₀	< 0.5 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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]
BaF3	IC₅₀	0.303 3 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 3 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 3 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	> 10 3 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 3 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]
MDA-MB-453	IC₅₀	5.7 1 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	0.028 3 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 3 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
NCI-H1975	IC₅₀	0.61 3 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]
SK-BR-3	IC₅₀	0.015 3 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 3 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 3 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 3 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]
Sf9	IC₅₀	< 0.001 3 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]

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.

Molekulargewicht

369.22

Formel

C₁₇H₁₃BrN₄O

CAS. Nr.

194423-15-9

Appearance

Solid

Color

Light yellow to khaki

SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molaritätsrechner
Verdünnungsrechner

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline 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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 98.01%

Select Batch:

Data Sheet (276 KB) SDS (392 KB)

COA (251 KB) HNMR (198 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

Verweise

[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]

Complete Stock Solution Preparation Table

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

PD168393 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:

PD168393194423-15-9PD 168393PD-168393EGFRAutophagyApoptosisEpidermal growth factor receptorErbB-1HER1MDA-MB-453tumorepidermoid carcinomaPDGFRFGFRInhibitorinhibitorinhibit

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PD168393

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Complete Stock Solution Preparation Table

PD168393 Related Classifications

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