379231-04-6
基本信息
N-(5-氯-1,3-苯并二氧戊環(huán)-4-基)-7-[2-(4-甲基-1-哌嗪基)乙氧基]-5-[(四氫-2H-吡喃-4-基)氧基]-4-喹唑啉胺
AZD0530 difuMarate
AZD0530(Saracatinib)
Saracatinib (AZD0530)
4-(6-Chloro-2,3-methylenedioxyanilino)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-tetrahydropyran-4-yloxyquinazoline
N-(5-Chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine
7-[2-[4-Methylpiperazin-1-yl]ethoxy]-5-[[tetrahydropyran-4-yl]oxy]-4-[[6-chloro-2,3-Methylenedioxyphenyl]aMino]quinazoline
N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine
N-(5-Chlorobenzo[d][1,3]dioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine
4-Quinazolinamine, N-(5-chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methyl-1-piperazinyl)ethoxy)-5-((tetrahydro-2H-pyran-4-yl)oxy)-
物理化學(xué)性質(zhì)
常見問(wèn)題列表
Target | Value |
c-Src
(Cell-free assay) | 2.7 nM |
LCK
(Cell-free assay) | <4 nM |
c-YES
(Cell-free assay) | 4 nM |
EGFR (L861Q)
(Cell-free assay) | 4 nM |
Lyn
(Cell-free assay) | 5 nM |
Saracatinib也有效抑制其他Src酪氨酸激酶家族成員,包括c-Yes, Fyn, Lyn, Blk, Fgr, 和Lck,IC50為4到10 nM。Saracatinib有效抑制SrcY530F突變的NIH 3T3細(xì)胞,IC50為80 nM。在NBT-II膀胱癌細(xì)胞中,Saracatinib顯著阻斷HT1080細(xì)胞通過(guò)立體骨膠原基質(zhì)的入侵,且完全抑制EGF誘導(dǎo)的細(xì)胞分散。Saracatinib作用于DU145和PC3細(xì)胞,通過(guò)抑制Y419磷酸化而有效抑制Src激活。Saracatinib抑制前列腺癌包括PC3, DU145, CWR22Rv1和 LNCaP的生長(zhǎng),而Saracatinib作用于 LAPC-4, PZ-HPV7和RWPE-1細(xì)胞時(shí)卻顯示低活性。Saracatinib使細(xì)胞周期停止在G1/S期,但是不使caspase 3斷裂。Saracatinib 也明顯抑制Boyden 小室的DU145和PC3 移動(dòng)。Saracatinib有效且持久抑制Akt,且增強(qiáng)A549和Calu-6細(xì)胞對(duì)放射處理的敏感性。Saracatinib在活性,再吸收,及組成上抑制蝕骨細(xì)胞。Saracatinib也可逆阻斷蝕骨細(xì)胞前體的移動(dòng)。
Saracatinib作用于Src3T3異體移植物顯示出強(qiáng)的腫瘤生長(zhǎng)抑制率,且Saracatinib造成Calu-6, MDA-MB-231, AsPc-1和BT474C移植瘤生長(zhǎng)適當(dāng)延遲。Saracatinib處理常位DU145鼠,按鼠體重,每千克每天口服處理25mg Saracatinib,結(jié)果顯示出強(qiáng)的抗癌活性。