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Gefitinib

CAS: 184475-35-2 Formula: C22H24ClFN4O3 MW: 446.9 Appearance: A crystalline Solid Purity: 98%
Hazardous

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C-1251 250 mg
$68.11
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500 mg
$129.00
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1 g
$245.62
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5 g
$1,032.00
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Over-activity of the epidermal growth factor receptor-associated tyrosine kinase (EGFR-TK) has been associated with a number of cancers and thus TK inhibitors could be potential therapeutic agents to prevent malignant growth. Gefitinib is a selective inhibitor of EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-Ras breast cancer, and OVCAR-3 ovarian cancer cell lines with ICs ranging between 0.2-0.4M. By interfering with the intracellular kinase domain, gefitinib prevents EGFR auto-phosphorylation and prevents downstream signal transduction. Gefitinib has been used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval for this compound (Iressa) when a phase III trial failed to demonstrate an overall survival benefit. Gefitinib appears to be most efficacious in treating certain EGFR gene mutations that are prevalent in Asian populations.

Additional Information

Synonyms Iressa, ZD1839
Product # C-1251
CAS # 184475-35-2
Chemical Name N-(3-chloro-4fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Formula C22H24ClFN4O3
MW 446.9
Appearance A crystalline Solid
Purity 98%
Solubility Soluble in ethanol (0.3 mg/ml), DMSO (20 mg/ml) or DMF (20 mg/ml), which should be purged of inert gas. Gefitinib is sparingly soluble in aqueous buffers.(For more information, please read Cof A).
Melting Point 193-194 °C
Boiling Point 586.8±50.0 °C at 760 mmHg
Storage Temp -20°C
Therapeutic Area Oncological Disorders
Use An EGFR-tyrosine kinase inhibitor use in cancer

Additional Information

MDL Number MFCD04307832
ChemACX X1511922-9
InChI InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)
SMILES COc1cc2c(cc1OCCCN3CCOCC3)c(ncn2)Nc4ccc(c(c4)Cl)F

Additional Information

GHS Pictograms
UN #'S UN 3077
PACKING GROUP III
Handling Room temperature

Additional Information

Certificate of Analysis 1 C-1251_C-1251,_D1035.pdf
Certificate of Analysis 2 C-1251_C-1251,_C1267.pdf
Certificate of Analysis 3 C-1251_C-1251,_C1267A.pdf

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Gefitinib

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