Home Cell Cycle BMI-1 inhibitor PTC-028 For research use only.

PTC-028

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.

PTC-028 Chemical Structure

PTC-028 Chemical Structure

CAS No. 1782970-28-8

Purity & Quality Control

Batch: S866201 DMSO]81 mg/mL]false]Ethanol]17 mg/mL]false]Water]Insoluble]false Purity: 99.76%
99.76

PTC-028 Related Products

Biological Activity

Description PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification.
Targets
BMI-1 [1]
In vitro
In vitro

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification. PTC-028 treatment selectively inhibits cancer cells in clonal growth and viability assays, whereas normal cells remain unaffected. Hyperphosphorylation-mediated depletion of cellular BMI-1 by PTC-028 coupled with a concurrent temporal decrease in ATP and a compromised mitochondrial redox balance potentiates caspase-dependent apoptosis[1].
Cell Research Cell lines Immortalized ovarian surface epithelium (OSE) or the fallopian tube epithelium(FTE) cells and ovarian cancer cells
Concentrations 0-500 nmol/L
Incubation Time 48 h
Method

Cells are treated with PTC-028 at the indicated concentrations for 48 hours and cellular viability is assessed using the MTS assay.
In Vivo
In vivo

In vivo, orally administered PTC-028, as a single agent, exhibits significant antitumor activity comparable with the standard therapy in an orthotopic mouse model of ovarian cancer. After administration of single oral doses to the CD-1 mice, total plasma AUC0-24h are 10.9 and 26.1 mg/h/mL at doses of 10 and 20 mg/kg, showing dose proportional pharmacokinetics. The Cmax for PTC-028 at 10 and 20 mg/kg is 0.79 and 1.49 mg/mL, respectively. The Cmax is reached at both dose levels 1-hour postdose after which plasma concentrations slowly reduce[1].
Animal Research Animal Models Preclinical model of ovarian cancer (NCr-nu mcie; 6 to 8 weeks old)
Dosages 10 mg/kg and 20 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 405.32 Formula

C19H12F5N5
CAS No. 1782970-28-8 SDF Download PTC-028 SDF
Smiles CC1=NC2=CC(=C(C=C2N1C3=NC(=CN=C3)NC4=CC=C(C=C4)C(F)(F)F)F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (199.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy PTC-028 | PTC-028 supplier | purchase PTC-028 | PTC-028 cost | PTC-028 manufacturer | order PTC-028 | PTC-028 distributor