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PTC-028 BMI-1 inhibitor

Name: PTC-028
SKU: S8662
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8662

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

Chemical Structure

Molecular Weight: 405.32

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.76

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 LIM kinase Nur77 APC
Related Products	PTC-209 PTC-209 HBr Unesbulin (PTC596) Bmi1 Antibody [F9A10] Bmi1 Antibody [D10D6]

Chemical Information, Storage & Stability

Molecular Weight	405.32	Formula	C₁₉H₁₂F₅N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1782970-28-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=NC2=CC(=C(C=C2N1C3=NC(=CN=C3)NC4=CC=C(C=C4)C(F)(F)F)F)F

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (199.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.050mg/ml (5.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 41 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.680mg/ml (1.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	BMI-1 ^[1]
In vitro	PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification. This compound treatment selectively inhibits cancer cells in clonal growth and viability assays, whereas normal cells remain unaffected. Hyperphosphorylation-mediated depletion of cellular BMI-1 by this agent coupled with a concurrent temporal decrease in ATP and a compromised mitochondrial redox balance potentiates caspase-dependent apoptosis^[1].
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 AUC_0-24h are 10.9 and 26.1 mg/h/mL at doses of 10 and 20 mg/kg, showing dose proportional pharmacokinetics. The Cmax for this compound 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].
References	[1] https://pubmed.ncbi.nlm.nih.gov/29158468/

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