Gefitinib (ZD1839) - Moligand™, 10mM in DMSO , Epidermal growth factor receptor erbB1 inhibitor, CAS No.184475-35-2, Epidermal growth factor receptor erbB1 inhibitor

CAS: 184475-35-2 Cat. No.: G408705 Molecular Weight: 446.9 EC Number: 643-034-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Iressa

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

In vitro

Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone..

In vivo

Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment.
Cell Data

cell lines：U87MG, A549 and H838 cells

Concentrations：0-2 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Synonyms

Iressa

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Epidermal growth factor receptor erbB1 inhibitor

Product Properties

• ALogP: 4.1

Names and Identifiers

• Isomeric SMILES: COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
• Molecular Weight: 446.9
• Reaxy-Rn: 8949523
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8949523&ln=

Associated Targets(Human)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 (3 Activities)

Discover Target: ERBB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor (128 Activities)

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GAK Tchem Cyclin-G-associated kinase (7 Activities)

Discover Target: GAK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RELA Tchem Transcription factor p65 (1 Activities)

Discover Target: RELA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 (1 Activities)

Discover Target: RIPK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCG2 Tchem ATP-binding cassette sub-family G member 2 (1 Activities)

Discover Target: ABCG2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 51 mg/mL (198.98 mM); Ethanol: 51 mg/mL (198.98 mM); Water: Insoluble
• Specific Rotation[α]: 1.62
• Boil Point(°C): 586.8 °C
• Melt Point(°C): 194.0 to 198.0 °C

References

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