Art. -Nr.: HY-14346

PD153035

(Synonyms: SU-5271; AG1517; ZM 252868)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with K_i and IC₅₀ of 6 and 25 pM, respectively.

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Reinheit: 98.56%
CAS. Nr.: 153436-54-5
Formel: C₁₆H₁₄BrN₃O₂
Molecular Weight:360.21

Speicherung:

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

PD153035 Chemical Structure

CAS. Nr.: 153436-54-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with K_i and IC₅₀ of 6 and 25 pM, respectively.

IC₅₀ & Target^[1]

EGFR

6 pM (Ki)

EGFR

25 pM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.004 μM Compound: 9d	Inhibition of epidermal growth factor receptor (EGF-R) autophosphorylation in A431 cells Inhibition of epidermal growth factor receptor (EGF-R) autophosphorylation in A431 cells	10.1016/S0960-894X(97)10117-2
A-431	IC₅₀	0.025 nM Compound: 14	Inhibition of the phosphorylation of a random polyglutamic acid/tyrosine copolymer by human epidermal growth factor receptor(EGFR) prepared from human A431 carcinoma cells Inhibition of the phosphorylation of a random polyglutamic acid/tyrosine copolymer by human epidermal growth factor receptor(EGFR) prepared from human A431 carcinoma cells	[PMID: 9154973]
A-431	IC₅₀	0.025 nM Compound: 32	Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles	[PMID: 8568816]
A-431	IC₅₀	0.025 nM Compound: 4	Inhibition of tyrosine kinase activity of Epidermal growth factor receptor from human A431 cells Inhibition of tyrosine kinase activity of Epidermal growth factor receptor from human A431 cells	[PMID: 8632415]
A-431	IC₅₀	0.029 nM Compound: 3	Evaluation of inhibitory activity against phospholipase C-gamma1 phosphorylation by Epidermal growth factor receptor enzyme isolated from A431 cells. Evaluation of inhibitory activity against phospholipase C-gamma1 phosphorylation by Epidermal growth factor receptor enzyme isolated from A431 cells.	[PMID: 7658435]
A-431	IC₅₀	0.029 nM Compound: 3	Inhibitory potency against isolated epidermal growth factor receptor (EGFR) from human A431 carcinoma cells Inhibitory potency against isolated epidermal growth factor receptor (EGFR) from human A431 carcinoma cells	[PMID: 8627606]
A-431	IC₅₀	0.03 μM Compound: PD-153035	Inhibition of EGF-stimulated tyrosine phosphorylation in A431 cells. Inhibition of EGF-stimulated tyrosine phosphorylation in A431 cells.	[PMID: 9357527]
A-431	IC₅₀	0.2 μM Compound: 17, PD-153035	Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA	[PMID: 19748785]
A-431	IC₅₀	0.2 μM Compound: 20, PD-153035	Inhibition of EGF-induced EGFR autophosphorylation in human A431 cells incubated for 60 mins prior to EGF-induction measured after 10 mins by phosphotyrosine ELISA Inhibition of EGF-induced EGFR autophosphorylation in human A431 cells incubated for 60 mins prior to EGF-induction measured after 10 mins by phosphotyrosine ELISA	[PMID: 22370340]
A-431	IC₅₀	0.2 μM Compound: 21, PD153035	Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA	[PMID: 23434139]
A-431	IC₅₀	0.2 μM Compound: 49, PD-153035	Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA	[PMID: 20403700]
A-431	IC₅₀	0.23 μM Compound: 13, PD-153035	Inhibition of EGFR in human A431 cells by phosphotyrosine cell-based ELISA Inhibition of EGFR in human A431 cells by phosphotyrosine cell-based ELISA	[PMID: 20092323]
A-431	IC₅₀	0.23 μM Compound: 18, PD-153035	Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA	[PMID: 22739090]
A-431	IC₅₀	0.23 μM Compound: 20, PD-153035	Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA	[PMID: 22204741]
A-431	IC₅₀	0.23 μM Compound: 25, PD153035	Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis	[PMID: 23375090]
A-431	IC₅₀	0.23 μM Compound: 19, PD-153035	Inhibition of EGFR expressed in human A431 cells Inhibition of EGFR expressed in human A431 cells	[PMID: 20558072]
A-431	IC₅₀	1.52 μM Compound: 63	Concentration needed to inhibit 50% growth of the human A431 (epidermoid carcinoma) cell lines Concentration needed to inhibit 50% growth of the human A431 (epidermoid carcinoma) cell lines	[PMID: 10966743]
A-431	IC₅₀	12.6 μM Compound: 17, PD-153035	Cytotoxicity against human A431 cells after 48 hrs by CYQUANT cell proliferation assay Cytotoxicity against human A431 cells after 48 hrs by CYQUANT cell proliferation assay	[PMID: 19748785]
A-431	IC₅₀	12.6 μM Compound: 20, PD-153035	Cytotoxicity against human A431 cells overexpressing EGFR incubated for 12 hrs measured after 36 hrs by CYQUANT assay Cytotoxicity against human A431 cells overexpressing EGFR incubated for 12 hrs measured after 36 hrs by CYQUANT assay	[PMID: 22370340]
A-431	IC₅₀	12.6 μM Compound: 25, PD153035	Cytotoxicity against human A431 cells overexpressing EGFR assessed as inhibition of cell proliferation treated for 12 hrs measured after 36 hrs by CYQUANT dye based assay Cytotoxicity against human A431 cells overexpressing EGFR assessed as inhibition of cell proliferation treated for 12 hrs measured after 36 hrs by CYQUANT dye based assay	[PMID: 23375090]
A-431	IC₅₀	12.6 μM Compound: 7, PD-153035	Cytotoxicity against human A431 cells Cytotoxicity against human A431 cells	[PMID: 20403693]
A-431	IC₅₀	12.6 μM Compound: PD-153035	Cytotoxicity against human A431 cells Cytotoxicity against human A431 cells	[PMID: 18467105]
A-431	IC₅₀	2.26 μg/mL Compound: PD-153035	Antiproliferative activity against human A431 cells after 24 to 48 hrs by WST1 assay Antiproliferative activity against human A431 cells after 24 to 48 hrs by WST1 assay	[PMID: 22901387]
A-431	IC₅₀	26.29 μM Compound: 1, PD-153035	Reversibility of antiproliferative activity against human A431 cells after recovery for 68 hrs by MTT assay Reversibility of antiproliferative activity against human A431 cells after recovery for 68 hrs by MTT assay	[PMID: 17154492]
A-431	IC₅₀	29 pM Compound: 3	Inhibition of Epidermal growth factor receptor from human A431 cell membranes Inhibition of Epidermal growth factor receptor from human A431 cell membranes	[PMID: 8627606]
A-431	IC₅₀	4.4 μM Compound: PD153035	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: 23900004]
A-431	IC₅₀	4.4 μM Compound: PD-153035	Cytotoxicity against human A431 cells after 72 hrs by MTT assay Cytotoxicity against human A431 cells after 72 hrs by MTT assay	[PMID: 20095624]
A-431	IC₅₀	8.31 μM Compound: 1, PD-153035	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]
A549	IC₅₀	8.13 μg/mL Compound: PD-153035	Antiproliferative activity against human A549 cells after 24 to 48 hrs by WST1 assay Antiproliferative activity against human A549 cells after 24 to 48 hrs by WST1 assay	[PMID: 22901387]
B16-F10	IC₅₀	1.74 μg/mL Compound: PD-153035	Antiproliferative activity against mouse B16F10 cells after 24 to 48 hrs by WST1 assay Antiproliferative activity against mouse B16F10 cells after 24 to 48 hrs by WST1 assay	[PMID: 22901387]
Balb/MK	IC₅₀	0.2 μM Compound: PD-153035	Inhibition of proliferation of EGF-dependent BALB/MK cells. Inhibition of proliferation of EGF-dependent BALB/MK cells.	[PMID: 9357527]
Bcap37	IC₅₀	13.7 μM Compound: PD-153035	Growth inhibition of human Bcap37 cells after 72 hrs by MTT assay Growth inhibition of human Bcap37 cells after 72 hrs by MTT assay	[PMID: 17681471]
Bcap37	IC₅₀	15.7 μM Compound: PD153035	Growth inhibition of human Bcap37 cells after 72 hrs by MTT assay Growth inhibition of human Bcap37 cells after 72 hrs by MTT assay	[PMID: 23811258]
Bcap37	IC₅₀	15.7 μM Compound: PD153035	Antiproliferative activity against human Bcap37 cells by MTT assay Antiproliferative activity against human Bcap37 cells by MTT assay	[PMID: 24583357]
Bcap37	IC₅₀	8.9 μM Compound: PD-153035	Antitumor activity against human Bcap37 cells by MTT method Antitumor activity against human Bcap37 cells by MTT method	[PMID: 17317179]
BGC-823	IC₅₀	14.4 μM Compound: PD153035	Growth inhibition of human BGC823 cells after 72 hrs by MTT assay Growth inhibition of human BGC823 cells after 72 hrs by MTT assay	[PMID: 23811258]
BGC-823	IC₅₀	14.4 μM Compound: PD153035	Antiproliferative activity against human BGC823 cells by MTT assay Antiproliferative activity against human BGC823 cells by MTT assay	[PMID: 24583357]
BGC-823	IC₅₀	16.8 μM Compound: PD-153035	Growth inhibition of human BGC823 cells after 72 hrs by MTT assay Growth inhibition of human BGC823 cells after 72 hrs by MTT assay	[PMID: 17681471]
BGC-823	IC₅₀	6.9 μM Compound: PD-153035	Antitumor activity against human BGC823 cells by MTT method Antitumor activity against human BGC823 cells by MTT method	[PMID: 17317179]
BGC-823	IC₅₀	6.9 μM Compound: PD-153035	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 20817326]
EA.hy 926	IC₅₀	7.1 μM Compound: 3a, PD-153035	Antiproliferative activity against human EAhy926 cells at 10 uM after 72 hrs by MTS assay Antiproliferative activity against human EAhy926 cells at 10 uM after 72 hrs by MTS assay	[PMID: 21353546]
HEK293	IC₅₀	260 nM Compound: 13; CA336	Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells measured after 2 hrs by nanoBRET assay Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells measured after 2 hrs by nanoBRET assay	[PMID: 30973735]
HeLa	IC₅₀	>10 μM Compound: PD153035	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 23900004]
HT-29	IC₅₀	>10 μM Compound: PD153035	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23900004]
HT-29	IC₅₀	10.1 μM Compound: 1a, PD-153035	Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay	[PMID: 21033670]
HT-29	IC₅₀	10.1 μM Compound: 3a, PD-153035	Antiproliferative activity against human HT-29 cells at 10 uM after 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells at 10 uM after 72 hrs by MTS assay	[PMID: 21353546]
HUVEC	IC₅₀	4.06 μM Compound: PD153035	Antiproliferative activity against HUVEC after 72 hrs by MTT assay Antiproliferative activity against HUVEC after 72 hrs by MTT assay	[PMID: 23900004]
MCF7	IC₅₀	3.21 μg/mL Compound: PD-153035	Antiproliferative activity against human MCF7 cells after 24 to 48 hrs by WST1 assay Antiproliferative activity against human MCF7 cells after 24 to 48 hrs by WST1 assay	[PMID: 22901387]
MCF7	IC₅₀	4.7 μM Compound: 1a, PD-153035	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay	[PMID: 21033670]
MCF7	IC₅₀	4.7 μM Compound: 3a, PD-153035	Antiproliferative activity against human MCF7 cells at 10 uM after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells at 10 uM after 72 hrs by MTS assay	[PMID: 21353546]
MDA-MB-468	IC₅₀	0.68 μM Compound: 16; PD153036	Inhibition of EGFR in human MDA-MB-468 cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter method Inhibition of EGFR in human MDA-MB-468 cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter method	[PMID: 30878832]
MDCK-II	IC₅₀	1.73 μM Compound: 43, PD153035	Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay	[PMID: 24184213]
MDCK-II	IC₅₀	2.32 μM Compound: 43, PD153035	Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry	[PMID: 24184213]
NIH3T3	IC₅₀	>10 μM Compound: PD153035	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 23900004]
NIH3T3	IC₅₀	>10 μM Compound: PD-153035	Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 20095624]
PC-3	IC₅₀	>10 μM Compound: 1a, PD-153035	Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay	[PMID: 21033670]
PC-3	IC₅₀	13.7 μM Compound: PD-153035	Antitumor activity against human PC3 cells by MTT method Antitumor activity against human PC3 cells by MTT method	[PMID: 17317179]
PC-3	IC₅₀	13.7 μM Compound: PD-153035	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 20817326]
PC-3	IC₅₀	8.3 μM Compound: PD153035	Growth inhibition of human PC3 cells after 72 hrs by MTT assay Growth inhibition of human PC3 cells after 72 hrs by MTT assay	[PMID: 23811258]
PC-3	IC₅₀	8.3 μM Compound: PD153035	Antiproliferative activity against human PC3 cells by MTT assay Antiproliferative activity against human PC3 cells by MTT assay	[PMID: 24583357]
PC-3	IC₅₀	8.9 μM Compound: PD-153035	Growth inhibition of human PC3 cells after 72 hrs by MTT assay Growth inhibition of human PC3 cells after 72 hrs by MTT assay	[PMID: 17681471]
SK-BR-3	IC₅₀	0.82 μM Compound: 63	Concentration needed to inhibit 50% growth of human SKBr3 (breast carcinoma) cell lines Concentration needed to inhibit 50% growth of human SKBr3 (breast carcinoma) cell lines	[PMID: 10966743]
SW-620	IC₅₀	13.94 μM Compound: 63	Concentration needed to inhibit 50% growth of human SW620 (colon carcinoma) cell lines Concentration needed to inhibit 50% growth of human SW620 (colon carcinoma) cell lines	[PMID: 10966743]

In Vitro

PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC₅₀ of 14 nM^[1]. PD153035 (SU 5271) has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD153035 (SU 5271) rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation^[2]. PD153035 (SU 5271) causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC₅₀ is less than 1 pM in most cases^[3].

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

In Vivo

PD153035 (SU 5271) levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD153035 (SU 5271) falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors^[4].

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

Chemical Information

CAS. Nr. 153436-54-5
Appearance Solid
Molecular Weight 360.21
Formel C₁₆H₁₄BrN₃O₂
Color White to off-white
SMILES

COC1=C(C=C(C2=C1)N=CN=C2NC3=CC(Br)=CC=C3)OC
Synonyms

SU-5271; AG1517; ZM 252868
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

Publications (10)

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Nat Commun

Composite regulation of ERK activity dynamics underlying tumour-specific traits in the intestine. [Abstract]

2018 Jun 5;9(1):2174. PMID: 29872037
Cell Death Dis

Activation of the JNKs/ATM-p53 axis is indispensable for the cytoprotection of dermal fibroblasts exposed to UVB radiation. [Abstract]

2022 Jul 25;13(7):647. PMID: 35879280
Elife

Intercellular propagation of extracellular signal-regulated kinase activation revealed by in vivo imaging of mouse skin. [Abstract]

2015 Feb 10:4:e05178. PMID: 25668746
Biochim Biophys Acta Mol Basis Dis

Targeting scleral remodeling and myopia development in form deprivation myopia through inhibition of EFEMP1 expression. [Abstract]

2024 Mar;1870(3):166981. PMID: 38101653
Sci Rep

Enhancement of melanoma aggressiveness via p38-MAPK, HIF-1α pathways, and metabolic reprogramming induced by Candida albicans. [Abstract]

2025 Nov 17;15(1):40227. PMID: 41249785
Int J Stem Cells

Generation of Urothelial Cells from Mouse-Induced Pluripotent Stem Cells. [Abstract]

2022 Nov 30;15(4):347-358. PMID: 35769056
Gen Comp Endocrinol

Stimulatory roles of epidermal growth factor receptor (EGFR) in ovarian development of mud crab Scylla paramamosain. [Abstract]

2020 Dec 1;299:113616. PMID: 32950581
J Toxicol Sci

Lead suppresses perlecan expression via EGFR-ERK1/2-COX-2-PGI2 pathway in cultured bovine vascular endothelial cells. [Abstract]

2023 Nov 14;48(12):655-663. PMID: 38044127
bioRxiv

2025 January 18.
bioRxiv

2024 Apr 4.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (92.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.7762 mL

13.8808 mL

27.7616 mL

5 mM

0.5552 mL

2.7762 mL

5.5523 mL

10 mM

0.2776 mL

1.3881 mL

2.7762 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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:

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

Protokoll

Cell Assay^[3]

Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed^[3].

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

Animal Administration^[3]

Mice: Mice are injected with PD153035 (SU 5271) (80 mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD153035 (SU 5271) of the EGF-stimulation^[3].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
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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)

Verweise

[1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76. [Content Brief]

[2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5. [Content Brief]

[3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106. [Content Brief]

[4]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302. [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	2.7762 mL	13.8808 mL	27.7616 mL	69.4040 mL
	5 mM	0.5552 mL	2.7762 mL	5.5523 mL	13.8808 mL
	10 mM	0.2776 mL	1.3881 mL	2.7762 mL	6.9404 mL
	15 mM	0.1851 mL	0.9254 mL	1.8508 mL	4.6269 mL
	20 mM	0.1388 mL	0.6940 mL	1.3881 mL	3.4702 mL
	25 mM	0.1110 mL	0.5552 mL	1.1105 mL	2.7762 mL
	30 mM	0.0925 mL	0.4627 mL	0.9254 mL	2.3135 mL
	40 mM	0.0694 mL	0.3470 mL	0.6940 mL	1.7351 mL
	50 mM	0.0555 mL	0.2776 mL	0.5552 mL	1.3881 mL
	60 mM	0.0463 mL	0.2313 mL	0.4627 mL	1.1567 mL
	80 mM	0.0347 mL	0.1735 mL	0.3470 mL	0.8675 mL

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PD153035

10 Cited Publications

100 mg Angebot einholen

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PD153035

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

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Protein Tyrosine Kinase Compound Library

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Differentiation Inducing Compound Library

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Publications Citing Use of MedChemExpress (MCE) PD153035

Alle EGFR Isoform-spezifische Produkte anzeigen

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Complete Stock Solution Preparation Table

PD153035 Related Classifications

HY-14346 Related Classifications