PZ0197

Pelitinib

≥98% (HPLC)

• Synonym(s): (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide, EKB 569, EKB-569, WAY-EKB-569
• Empirical Formula (Hill Notation): C₂₄H₂₃ClFN₅O₂
• CAS Number: 257933-82-7
• Molecular Weight: 467.92
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated; protect from light
• color: white to beige
• solubility: DMSO: 5 mg/mL, clear (warmed)
• storage temp.: −20°C
• SMILES string: Fc1c(cc(cc1)Nc2c3c(ncc2C#N)cc(c(c3)NC(=O)\C=C\CN(C)C)OCC)Cl
• InChI: 1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+
• InChI key: WVUNYSQLFKLYNI-AATRIKPKSA-N

Description

Biochem/physiol Actions

Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC₅₀ about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.

Pelitinib specifically targets cancer cells with elevated expression of the efflux transporters ATP-binding cassette (ABC)B1/ABCG2 post hyperthermia. This property of peltinib aids in the elimination of metastasis and prevention of cancer recurrence.

Other Notes

Light sensitive

Safety Information

• Pictograms: GHS06
• Signal Word: Danger
• Hazard Statements: H301
• Precautionary Statements: P264 - P270 - P301 + P310 - P405 - P501
• Hazard Classifications: Acute Tox. 3 Oral
• Storage Class Code: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable