SML3195

AZD0530

≥98% (HPLC)

• Synonym(s): 4-(6-Chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline, 7-[2-[4-Methylpiperazin-1-yl]ethoxy]-5-[[tetrahydropyran-4-yl]oxy]-4-[[6-chloro-2,3-methylenedioxyphenyl]amino]quinazoline, AZD 0530, AZD-0530, N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine, Saracatinib
• Empirical Formula (Hill Notation): C₂₇H₃₂ClN₅O₅
• CAS Number: 379231-04-6
• Molecular Weight: 542.03
• MDL number: MFCD09832698
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• InChI: 1S/C27H32ClN5O5/c1-32-6-8-33(9-7-32)10-13-35-19-14-21-24(23(15-19)38-18-4-11-34-12-5-18)27(30-16-29-21)31-25-20(28)2-3-22-26(25)37-17-36-22/h2-3,14-16,18H,4-13,17H2,1H3,(H,29,30,31)
• InChI key: OUKYUETWWIPKQR-UHFFFAOYSA-N

Description

Biochem/physiol Actions

AZD0530 is an orally active, potent tyrosine kinase inhibitor against Src family kinases (IC50 = 2.7 nM/c-Src, <4 nM/Lck, 4 nM/c-Yes, 5 nM/Lyn, 10 nM/Fyn, 10 nM/Fgr, 11 nM/Blk), v-Abl (IC50 = 30 nM) and EGFR (L861Q/L858R/wt IC50 = 4/5/66 nM). AZD0530 exhibits anti-proliferation activity in cancer cultures (IC50 = 80-700 nM; Src Y530F NIH 3T3, LoVo, K562, PC-9, SW 403, PC-3) and shows efficacy against several human tumor xenograft growth in mice in vivo (6.25-50 mg/kg/day p.o.; MDA-MB-231, AsPc-1, Calu-6, BT474C).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable