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801991-87-7

中文名稱 ZZW-115
英文名稱 1-Piperazineethanamine, N,N-dimethyl-4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]-
CAS 801991-87-7
分子式 C24H31F3N4S
分子量 464.59
MOL 文件 801991-87-7.mol
更新日期 2024/11/16 21:40:38
801991-87-7 結(jié)構(gòu)式 801991-87-7 結(jié)構(gòu)式

基本信息

英文別名
ZZW-115
1-Piperazineethanamine, N,N-dimethyl-4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]-

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存

常見(jiàn)問(wèn)題列表

生物活性
ZZW-115 是一種有效的 NUPR1 抑制劑,Kd 為 2.1 μM,通過(guò)壞死和凋亡 (apoptosis) 誘導(dǎo)腫瘤細(xì)胞死亡。具有抗癌活性。
體外研究

ZZW-115 (0.1-33 μM; 72 hours) is efficient in killing cancer cells, with an IC 50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14).
ZZW-115 (0-100 μM; 24-72 hours) is efficient to kill these tumor cells with an IC 50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells).
ZZW-115 induces pancreatic cell death by necrosis and apoptosis. ZZW-115 treatment induces a decrease in ATP production and induces a ROS overproduction.
LDH release is significantly higher in ZZW-115-treated cells (MiaPaCa-2, 02-063, LIPC, Foie8b, and HN14 cells) than in control cells in a concentration-dependent manner. Similarly, caspase 3/7 activity is also greater in ZZW-115-treated cells. These experiments demonstrated that ZZW-115 exerted both pronecrotic and proapoptotic effects.

Cell Viability Assay

Cell Line: ANOR cells, MiaPaCa-2, 02-063, 01008, LIPC, 02136, HN01,01046, AOIPC, Foie8b, HN14 cells
Concentration: 0.1- 33 μM
Incubation Time: 72 hours
Result: Was efficient in killing cancer cells, with an IC 50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14).

Cell Proliferation Assay

Cell Line: U87, A375, U2OS, SaOS-2, HT29, SK-CO-1, LS174T, H1299 and H358, HepG2, PC3, THP-1, Daudi, Jurkat and MDA-MB-231 cells
Concentration: 0-100 μM
Incubation Time: 24 or 72 hours
Result: Was efficient to kill these tumor cells with an IC 50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells).
體內(nèi)研究

ZZW-115 (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors.
ZZW-115 (5 mg/kg for 30 days; immunocompetent C57BL/6 mice were orthotopically implanted with Panc02 cells) treatment shows the tumor size is almost unmeasurable in some cases.

Animal Model: NMRI-Foxn1nu/Foxn1nu mice (nude mice) xenografted with MiaPaCa-2 cells
Dosage: 5, 2.5, 1.0, or 0.5 mg/kg
Administration: Injection, daily for 30 days
Result: When the mice were injected with 5 mg/kg ZZW-115, the tumors stopped growing a few days after treatment and their size decreased progressively, almost disappearing at the end of the treatment.
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