SML3872
AZ0108
≥98% (HPLC)
别名:
(S)-4-((3-(3-(1,1-difluoroethyl)-6-methyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)phenyl)difluoromethyl)phthalazin-1(2H)-one, 4-[[3-[[(6S)-3-(1,1-Difluoroethyl)-5,6-dihydro-6-methyl-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]carbonyl]phenyl]difluoromethyl]-1(2H)-phthalazinone, AZ 0108
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About This Item
推荐产品
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
-10 to -25°C
SMILES 字串
FC(C1=CC=CC(C(N2[C@@H](C)CN3C(C2)=NN=C3C(F)(F)C)=O)=C1)(F)C(C4=CC=CC=C45)=NNC5=O
生化／生理作用
Inhibitor of Poly (ADP-ribose) polymerase PARP1, 2, and 6.
AZ0108 is an inhibitor of Poly (ADP-ribose) polymerase PARP1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. It was shown to block centrosome clustering in HeLa cells with an EC50 value of 53 nM and kill a DLBCL lymphoma cancer cell line with a GI50 value of 17 nM. AZ0108 induces replication stress in tumorigenic cells.
AZ0108 is an inhibitor of Poly (ADP-ribose) polymerase PARP1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. It was shown to block centrosome clustering in HeLa cells with an EC50 value of 53 nM and kill a DLBCL lymphoma cancer cell line with a GI50 value of 17 nM. AZ0108 induces replication stress in tumorigenic cells.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering
Bioorganic & Medicinal Chemistry Letters, 25(24), 5743-5747 (2015)
Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer
Cancer research, 78(23), 6691-6702 (2018)
Allosteric regulation of DNA binding and target residence time drive the cytotoxicity of phthalazinone-based PARP-1 inhibitors
Cell Chemical Biology, 29(12) (2022)
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