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ZZW 115

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ZZW 115
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Cat #: V2523 CAS #: 801991-87-7 Purity ≥ 99%

Description: ZZW-115 (ZZW115) is a novel and potent NUPR1 inhibitor (Kd=2.1 uM) with antitumor activity. It is the most active one in the family of TFP-derived compounds. NUPR1 is an intrinsically disordered protein (IDP) with an entirely disordered conformation

References: Santofimia-Castaño P, et al. Ligand-based design identifies a potent NUPR1 inhibitor exerting anticancer activity via necroptosis. J Clin Invest. 2019;129(6):2500-2513. Published 2019 Mar 28.

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Molecular Weight (MW)464.59
Molecular FormulaC24H31F3N4S
CAS No.801991-87-7
SMILES CodeFC(C(C=C1N2CCCN3CCN(CCN(C)C)CC3)=CC=C1SC4=C2C=CC=C4)(F)F
SynonymsZZW 115; ZZW115; ZZW-115;
ProtocolIn VitroLDH 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. ZZW-115 induces pancreatic cell death by necrosis and apoptosis. ZZW-115 treatment induces a decrease in ATP production and induces a ROS overproduction. ZZW-115 (0-100 μM; 24-72 hours) is efficient to kill these tumor cells with an IC50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells). ZZW-115 (0.1-33 μM; 72 hours) is efficient in killing cancer cells, with an IC50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14).
In VivoZZW-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. ZZW-115 (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1524 mL10.7622 mL21.5244 mL43.0487 mL
5mM0.4305 mL2.1524 mL4.3049 mL8.6097 mL
10mM0.2152 mL1.0762 mL2.1524 mL4.3049 mL
20mM0.1076 mL0.5381 mL1.0762 mL2.1524 mL
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Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.