1-Piperazineethanamine, N,N-dimethyl-4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]-

Product Name1-Piperazineethanamine, N,N-dimethyl-4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]-
CAS801991-87-7
MFC24H31F3N4S
MW464.59
EINECS
MOL File801991-87-7.mol

Chemical Properties

storage temp.

Store at -20°C

Usage And Synthesis

Biological Activity

ZZW-115 is a potent NUPR1 inhibitor with Kd of 2.1 μM, which induces tumor cell death via necrosis and apoptosis. Has anticancer activity.

in vitro

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

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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).

in vivo

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 showed 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, the tumors stopped growing a few days after treatment and their size decreased progressively, almost disappearing at the end of the treatm ent.

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