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Safety Information

SML3195

Sigma-Aldrich

AZD0530

≥98% (HPLC)

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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:
Molecular Weight:
542.03
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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).

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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