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MedKoo Cat#: 531248 | Name: PD153035 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2).

Chemical Structure

PD153035 HCl
PD153035 HCl
CAS#183322-45-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 531248

Name: PD153035 HCl

CAS#: 183322-45-4 (HCl)

Chemical Formula: C16H15BrClN3O2

Exact Mass: 0.0000

Molecular Weight: 396.67

Elemental Analysis: C, 48.45; H, 3.81; Br, 20.14; Cl, 8.94; N, 10.59; O, 8.07

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
200mg USD 650.00 2 Weeks
500mg USD 1,250.00 2 Weeks
1g USD 2,150.00 2 Weeks
2g USD 3,750.00 2 Weeks
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Related CAS #
153436-54-5 (free base) 183322-45-4 (HCl) 205195-07-9 (xHCl) 586347-97-9 (nitrate)
Synonym
PD153035; PD 153035; PD-153035; PD153035 HCl; PD153035 hydrochloride.
IUPAC/Chemical Name
N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride
InChi Key
ZJOKWAWPAPMNIM-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H14BrN3O2.ClH/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11;/h3-9H,1-2H3,(H,18,19,20);1H
SMILES Code
COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 183322-45-4 (PD153035 HCl) 153436-54-5 (PD153035 free base)
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM.
In vitro activity:
A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF receptor tyrosine kinase and inhibited other purified tyrosine kinases only at micromolar or higher concentrations. PD 153035 rapidly suppressed autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocked EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. Reference: Science. 1994 Aug 19;265(5175):1093-5. https://pubmed.ncbi.nlm.nih.gov/8066447/
In vivo activity:
This study investigated whether inhibiting EGFR using the EGFR tyrosine kinase inhibitor (TKI) PD153035 improves NAFLD. These results demonstrate that EGFR was activated in liver tissues from high fat diet (HFD)-induced NAFLD mice. Inhibiting EGFR using PD153035 significantly reduced phosphatidylinositol-3-kinase/protein kinase B signaling and sterol responsive elementary binding protein 1 and 2 expression, which prevented HFD-induced hepatic steatosis and hypercholesterolemia by reducing de novo lipogenesis and cholesterol synthesis and enhancing fatty acid oxidation. Reference: PLoS One. 2019 Feb 8;14(2):e0210828. https://pubmed.ncbi.nlm.nih.gov/30735525/
Solvent mg/mL mM
Solubility
DMF 0.2 0.40
DMSO 2.0 4.94
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 396.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106. PMID: 9815602. 2. Fry DW, Kraker AJ, McMichael A, Ambroso LA, Nelson JM, Leopold WR, Connors RW, Bridges AJ. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5. doi: 10.1126/science.8066447. PMID: 8066447. 3. Choung S, Kim JM, Joung KH, Lee ES, Kim HJ, Ku BJ. Epidermal growth factor receptor inhibition attenuates non-alcoholic fatty liver disease in diet-induced obese mice. PLoS One. 2019 Feb 8;14(2):e0210828. doi: 10.1371/journal.pone.0210828. PMID: 30735525; PMCID: PMC6368280. 4. Kenessey I, Kramer Z, István L, Cserepes MT, Garay T, Hegedűs B, Dobos J, Tímár J, Tóvári J. Inhibition of epidermal growth factor receptor improves antitumor efficacy of vemurafenib in BRAF-mutant human melanoma in preclinical model. Melanoma Res. 2018 Dec;28(6):536-546. doi: 10.1097/CMR.0000000000000488. PMID: 30124539.
In vitro protocol:
1. Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106. PMID: 9815602. 2. Fry DW, Kraker AJ, McMichael A, Ambroso LA, Nelson JM, Leopold WR, Connors RW, Bridges AJ. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5. doi: 10.1126/science.8066447. PMID: 8066447.
In vivo protocol:
1. Choung S, Kim JM, Joung KH, Lee ES, Kim HJ, Ku BJ. Epidermal growth factor receptor inhibition attenuates non-alcoholic fatty liver disease in diet-induced obese mice. PLoS One. 2019 Feb 8;14(2):e0210828. doi: 10.1371/journal.pone.0210828. PMID: 30735525; PMCID: PMC6368280. 2. Kenessey I, Kramer Z, István L, Cserepes MT, Garay T, Hegedűs B, Dobos J, Tímár J, Tóvári J. Inhibition of epidermal growth factor receptor improves antitumor efficacy of vemurafenib in BRAF-mutant human melanoma in preclinical model. Melanoma Res. 2018 Dec;28(6):536-546. doi: 10.1097/CMR.0000000000000488. PMID: 30124539.
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Discovering the mechanism of action of drugs with a sparse explainable network. EBioMedicine. 2023 Sep;95:104767. doi: 10.1016/j.ebiom.2023.104767. Epub 2023 Aug 24. PMID: 37633093; PMCID: PMC10474372. 5: Ochora DO, Mogire RM, Masai RJ, Yeda RA, Mwakio EW, Amwoma JG, Wakoli DM, Yenesew A, Akala HM. Ex vivo and In vitro antiplasmodial activities of approved drugs predicted to have antimalarial activities using chemogenomics and drug repositioning approach. Heliyon. 2023 Aug 1;9(8):e18863. doi: 10.1016/j.heliyon.2023.e18863. PMID: 37583763; PMCID: PMC10424068. 6: Wang Q, Wang F, Li X, Ma Z, Jiang D. Quercetin inhibits the amphiregulin/EGFR signaling-mediated renal tubular epithelial-mesenchymal transition and renal fibrosis in obstructive nephropathy. Phytother Res. 2023 Jan;37(1):111-123. doi: 10.1002/ptr.7599. Epub 2022 Oct 11. PMID: 36221860. 7: Högnäsbacka A, Poot AJ, Vugts DJ, van Dongen GAMS, Windhorst AD. The Development of Positron Emission Tomography Tracers for In Vivo Targeting the Kinase Domain of the Epidermal Growth Factor Receptor. Pharmaceuticals (Basel). 2022 Apr 5;15(4):450. doi: 10.3390/ph15040450. PMID: 35455447; PMCID: PMC9033078. 8: Gbetuwa M, Lu LS, Wang TJ, Chen YJ, Chiou JF, Su TY, Yang TS. Nucleus Near- Infrared (nNIR) Irradiation of Single A549 Cells Induces DNA Damage and Activates EGFR Leading to Mitochondrial Fission. Cells. 2022 Feb 11;11(4):624. doi: 10.3390/cells11040624. PMID: 35203275; PMCID: PMC8870661. 9: Leonard NA, Reidy E, Thompson K, McDermott E, Peerani E, Tomas Bort E, Balkwill FR, Loessner D, Ryan AE. Stromal Cells Promote Matrix Deposition, Remodelling and an Immunosuppressive Tumour Microenvironment in a 3D Model of Colon Cancer. Cancers (Basel). 2021 Nov 29;13(23):5998. doi: 10.3390/cancers13235998. PMID: 34885111; PMCID: PMC8656544. 10: Bandara M, MacNaughton WK. Protease-activated receptor-2 activation enhances epithelial wound healing via epidermal growth factor receptor. Tissue Barriers. 2022 Apr 3;10(2):1968763. doi: 10.1080/21688370.2021.1968763. Epub 2021 Sep 11. PMID: 34511032; PMCID: PMC9067514. 11: Urban H, Maurer GD, Luger AL, Lorenz NI, Sauer B, Stroh C, Trojan J, Mittelbronn M, Steinbach JP, Harter PN, Ronellenfitsch MW. Cetuximab-Mediated Protection from Hypoxia- Induced Cell Death: Implications for Therapy Sequence in Colorectal Cancer. Cancers (Basel). 2020 Oct 20;12(10):3050. doi: 10.3390/cancers12103050. PMID: 33092032; PMCID: PMC7589936. 12: Lu B, Jiang Q, Liu A, Huang H, Ye H. Stimulatory roles of epidermal growth factor receptor (EGFR) in ovarian development of mud crab Scylla paramamosain. Gen Comp Endocrinol. 2020 Dec 1;299:113616. doi: 10.1016/j.ygcen.2020.113616. Epub 2020 Sep 17. PMID: 32950581. 13: Mehus AA, Bergum N, Knutson P, Shrestha S, Zhou XD, Garrett SH, Sens DA, Sens MA, Somji S. 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Novel anilino quinazoline-based EGFR tyrosine kinase inhibitors for treatment of non-small cell lung cancer. Biomater Sci. 2021 Jan 21;9(2):443-455. doi: 10.1039/d0bm00293c. Epub 2020 Apr 1. Erratum in: Biomater Sci. 2022 May 17;10(10):2720-2722. doi: 10.1039/d2bm90028a. PMID: 32236267. 17: Furue K, Ito T, Tanaka Y, Hashimoto-Hachiya A, Takemura M, Murata M, Kido- Nakahara M, Tsuji G, Nakahara T, Furue M. The EGFR-ERK/JNK-CCL20 Pathway in Scratched Keratinocytes May Underpin Koebnerization in Psoriasis Patients. Int J Mol Sci. 2020 Jan 9;21(2):434. doi: 10.3390/ijms21020434. PMID: 31936670; PMCID: PMC7013594. 18: Chang MC, Pan YH, Wu HL, Lu YJ, Liao WC, Yeh CY, Lee JJ, Jeng JH. Stimulation of MMP-9 of oral epithelial cells by areca nut extract is related to TGF-β/Smad2-dependent and -independent pathways and prevented by betel leaf extract, hydroxychavicol and melatonin. Aging (Albany NY). 2019 Dec 12;11(23):11624-11639. doi: 10.18632/aging.102565. Epub 2019 Dec 12. 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