PHY34

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PHY34 是一种有效的自噬抑制剂，通过抑制晚期自噬而产生细胞毒性作用（MDA-MB-435 IC50=23 nM，MDA-MB-231 IC50=5.2 nM）；破坏溶酶体功能，显着抑制中空纤维中癌细胞系的生长，并减少异种移植模型中的卵巢肿瘤负担。

PHY34 is a potent autophagy inhibitor with cytotoxic effects by inhibiting autophagy at a late stage (MDA-MB-435 IC50=23 nM, MDA-MB-231 IC50=5.2 nM); disrupts lysosomal function, significantly inhibits the growth of cancer cell lines in hollow fibers, as well as reduces ovarian tumor burden in a xenograft model.

Cell Viability Assay Cell Line:OVCAR8, OVCAR3, HT-29, MDA-MB-435, MDA-MB-231, IOSE80, FT33Concentration:0.001 nM-50 μM Incubation Time:72 h Result:Inhibited the growth of various cancer cells with IC50 values of 4 nM(OVCAR8, OVCAR3), 43.3 nM(HT-29) , 23 nM(MDA-MB-435) , 5.2 nM(MDA-MB-231).Exhibited no toxicity to IOSE80 and FT33 (IC50 >50 μM).Cell Viability Assay Cell Line:H4 Concentration:0.01 nM-2 μM Incubation Time:72 h Result:Inhibited mutant cell with an IC50 value of 246 pM that was 1000-fold more potent than HTP-013(434 nM).Conferred resistance in V8231 mutation and no impact activity in T216A mutation.Apoptosis Analysis Cell Line:OVCAR8, OVCAR3 Concentration:10 nM, 100 nM Incubation Time:72 h Result:Increased the number of cells in early and late apoptosis in OVCAR8 and OVCAR3 at 10 nM and 100 nM, respectively. Cell Autophagy Assay Cell Line:Hela Concentration:9.31 fM-20 μM Incubation Time:4 h Result:Sustained high levels of LC3B puncta with an EC50 value of 2 nM.Inhibited autophagy with an EC50 value of 3.9 nM.Cell Autophagy Assay Cell Line: OVCAR3 Concentration:5 nM Incubation Time:4 h Result:Inhibited autophagy with an ED50 value of 6.29 nM, and was more potent than bafilomycin A1 (HY-100558) with an ED50 value of 29.1 nM.Western Blot Analysis Cell Line:OVCAR8, OVCAR3, OVCAR4 Concentration:10 nM, 100 nM Incubation Time:48 h, 72 h Result: Increased cPARP levels in OVCAR8 after 48 h at 10 nM, in OVCAR4 and OVCAR3 after 72 h at 100 nM, respectively. Reversed the conversion of PARP to cPARP combined with RAP (HY-10219) of 1 μM.Western Blot Analysis Cell Line:OVCAR8, OVCAR3, OVCAR4 Concentration:10 nM Incubation Time:24 h, 48 h, 72 h Result:Promoted histone H3, LAMP1/2, ACSS2, and PCNA nuclear protein accumulation at 48 h.Reduced expression of KPNA2 (Karyopherin subunit alpha 2) with time-dependent manner.

Animal Model:OVCAR8-induced xenograft models in female nude mice.Dosage:0.75 mg/kg, three times a week for three weeks Administration:Intraperitoneal injection (i.p.)Result:Decreased tumor burden based on average abdominal radiant efficiency with no gross toxicity through analysis of fluorescence imaging.

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Autophagy

Autophagy

Autophagy

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2130033-55-3

522.506

C28H26O10

>98% (HPLC)

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CC1(OC2C(OC(C(C2O1)O)OC3=C4COC(=O)C4=C(C5=CC=CC=C53)C6=CC7=C(C=C6)OCO7)CO)C

9-(benzo[d][1,3]dioxol-5-yl)-4-(((3aS,4R,6S,7R,7aR)-7-hydroxy-4-(hydroxymethyl)-2,2-dimethyltetrahydro-4H-[1,3]dioxolo[4,5-c]pyran-6-yl)oxy)naphtho[2,3-c]furan-1(3H)-one

(-20℃)

With Ice Pack

≥ 2 years