PD153035 Hydrochloride
Based on 10 publication(s) in Google Scholar
PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.
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- Pureza: 99.48%
- No. CAS: 183322-45-4
- Fòrmula: C16H15BrClN3O2
- Peso molecular:396.67
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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Publications Citing Use of MedChemExpress (MCE) PD153035 Hydrochloride
More- Nat Commun. 2018 Jun 5;9(1):2174. [Abstract]
- Cell Death Dis. 2022 Jul 25;13(7):647. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Mar;1870(3):166981. [Abstract]
- Sci Rep. 2025 Nov 17;15(1):40227. [Abstract]
- Int J Stem Cells. 2022 Nov 30;15(4):347-358. [Abstract]
- Gen Comp Endocrinol. 2020 Dec 1:299:113616. [Abstract]
- J Toxicol Sci. 2023 Nov 14;48(12):655-663. [Abstract]
- bioRxiv. 2025 January 18.
- bioRxiv. 2024 Apr 4.
- Elife. 2015 Feb 10:4:e05178. [Abstract]
Ver todos los productos específicos de isoformas EGFR
More
Actividad biológica
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EGFR 6 pM (Ki) |
EGFR 25 pM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.66 nM
Compound: 11c
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Displacement of [125I]4-(3-iodoanilino)-6,7-dimethoxyquinazoline from EGFR tyrosine kinase in human A431 cell membranes
Displacement of [125I]4-(3-iodoanilino)-6,7-dimethoxyquinazoline from EGFR tyrosine kinase in human A431 cell membranes
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[PMID: 16279804] |
| BaF3 | IC50 |
143 nM
Compound: 11c
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Inhibition of human ErbB2 tyrosine kinase phosphorylation expressed in mouse BaF3 cells
Inhibition of human ErbB2 tyrosine kinase phosphorylation expressed in mouse BaF3 cells
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[PMID: 16279804] |
| BaF3 | IC50 |
2.6 nM
Compound: 11c
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Inhibition of human EGFR tyrosine kinase phosphorylation expressed in mouse BaF3 cells
Inhibition of human EGFR tyrosine kinase phosphorylation expressed in mouse BaF3 cells
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[PMID: 16279804] |
| MCF-10A | IC50 |
211 nM
Compound: 11c
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Inhibition of DNA synthesis in EGF-dependent human MCF10A cells assessed as [3H]thymidine incorporation
Inhibition of DNA synthesis in EGF-dependent human MCF10A cells assessed as [3H]thymidine incorporation
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[PMID: 16279804] |
| MCF7 | IC50 |
1613 nM
Compound: 11c
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Inhibition of DNA synthesis in EGF-independent human MCF7 cells assessed as 3H]thymidine incorporation
Inhibition of DNA synthesis in EGF-independent human MCF7 cells assessed as 3H]thymidine incorporation
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[PMID: 16279804] |
PD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM[1]. PD153035 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 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 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 183322-45-4
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Appearance Solid
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Peso molecular 396.67
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Fòrmula C16H15BrClN3O2
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Color Off-white to light yellow
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SMILES
COC1=C(C=C(C2=C1)N=CN=C2NC3=CC(Br)=CC=C3)OC.Cl
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Synonyms
SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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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 -
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
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 -
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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
Solvente y solubilidad
DMSO : 4 mg/mL (10.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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.
Mice: Mice are injected with PD153035 (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 PD 153035 of the EGF-stimulation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (642 KB)
- English - EN (642 KB)
- Français - FR (642 KB)
- Deutsch - DE (642 KB)
- Norwegian - NO (642 KB)
- Español - ES (642 KB)
- Swedish - SV (642 KB)
- Italian - IT (642 KB)
- Korean - KR (642 KB)
- Portuguese - PT (642 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 (sealed storage, away from moisture). 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 | 2.5210 mL | 12.6049 mL | 25.2099 mL | 63.0247 mL |
| 5 mM | 0.5042 mL | 2.5210 mL | 5.0420 mL | 12.6049 mL | |
| 10 mM | 0.2521 mL | 1.2605 mL | 2.5210 mL | 6.3025 mL |
PD153035 Hydrochloride Related Classifications
HY-12013 Related Classifications
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