379231-04-6

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AZD0530/Saracatinib,AZD0530 difumarate

379231-04-6

编号ABP000854 化学名称AZD0530/Saracatinib,AZD0530 difumarate 英文名称 AZD0530/Saracatinib,AZD0530 difumarate MDL: MFCD18837677 分子式C28H33ClN4O5 分子量541.045 纯度 99%

化学名称 : AZD0530/Saracatinib,AZD0530 difumarate

CAS : 379231-04-6

英文名称: AZD0530/Saracatinib,AZD0530 difumarate

英文同义词: 7-(2-(1-METHYLPIPERIDIN-4-YL)ETHOXY)-N-(5-CHLOROBENZO[D][1,3]DIOXOL-4-YL)-5-(TETRAHYDRO-2H-PYRAN-4-YLOXY)QUINAZOLIN-4-AMINE

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

WP1130 is a novel selective small molecular deubiquitinase (DUB) inhibitor and a Bcr/Abl destruction pathway activator with an IC50 of 1.8 μM for K562 cells. WP1130 acts as a partly selective deubiquitinases (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37, which are known to regulate survival protein stability and 26S proteasome function. WP1130-mediated inhibition of tumor-activated DUBs results in downregulation of antiapoptotic and upregulation of proapoptotic proteins, such as MCL-1 and p53. WP1130 specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells. WP1130 was more effective in reducing leukemic versus normal hematopoietic colony formation and strongly inhibited colony formation of cells derived from patients with T315I mutant Bcr/Abl-expressing CML in blast crisis. Collectively, WP1130 reduces wild-type and T315I mutant Bcr/Abl protein levels in CML cells through a unique mechanism and may be useful in treating CML.[1][2]

参考文献

[1] Bartholomeusz GA et al. Blood. 2007 Apr 15; 109(8):3470-8.

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