1. Apoptosis
  2. Apoptosis
  3. PTC-028

PTC-028 

Cat. No.: HY-103696 Purity: >98.0%
Handling Instructions

PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. Depletion of BMI-1 by PTC-028 induces caspase-mediated apoptosis.

For research use only. We do not sell to patients.

PTC-028 Chemical Structure

PTC-028 Chemical Structure

CAS No. : 1782970-28-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
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10 mg USD 180 In-stock
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25 mg USD 360 In-stock
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50 mg USD 610 In-stock
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100 mg USD 960 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. Depletion of BMI-1 by PTC-028 induces caspase-mediated apoptosis[1].

IC50 & Target

BMI-1[1]

In Vitro

PTC-028 (25-500 nM; 48 hours) significantly decreases CP20, OVCAR4 and OV90 epithelial ovarian cancer cells viability. However, in normal ovarian surface epithelial cells (OSE) and fallopian tube epithelial cells (FTE) cells, up to 500 nM treatment with PTC-028 for 48 hours has minimal effect (~18-30% decrease)[1].
PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. PTC-028 subsequently reduces BMI-1 in the biochemical functional readout [1].
uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged [1].
PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remains unchanged compared to that of the control [1].
Significant cleavage of Caspase 7, Caspase 9 and PARP is observed in PTC-028 (100 nM; 48 hours)[1].

Cell Viability Assay[1]

Cell Line: OVCAR4, OV90 and CP20 cells
Concentration: 0, 25, 50, 100, 200, 500 nM
Incubation Time: 48 hours
Result: OVCAR4, OV90 and CP20 cells demonstrated significant dose dependent decrease in cell viability with an IC50 of ~100 nM and ~95% decrease at 500 nM.

Western Blot Analysis[1]

Cell Line: OV90 and CP20 cells
Concentration: 100 nM
Incubation Time: 2, 4, 6, 12 hours
Result: A time-dependent increase in the phosphorylated BMI-1 species and subsequent reduction in the biochemical functional readout.
uH2A was observed up to 12 h while total H2A levels remained unchanged.
In Vivo

PTC-028 (15 mg/kg; administered orally twice weekly) causes ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].
No obvious toxicity is noted in the animals during therapy experiments as assessed by mean body weight[1].
PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The Cmax is reached at both dose levels 1h post dose after which plasma concentrations slowly reduce[1].

Animal Model: Female athymic nude mice with implanted OV90 cells[1]
Dosage: 15 mg/kg
Administration: Orally administered; twice weekly
Result: Caused ~94% (0.169 g) reduction in tumor weight.
Animal Model: Female CD-1 mice[1]
Dosage: 10 mg/kg or 20mg/kg
Administration: Oral administered; single dose
Result: Total plasma AUC0-24h were 10.9 and 26.1 μg•h/mL at doses of 10 and 20 mg/kg. The Cmax for PTC-028 at 10 and 20 mg/kg was 0.79 and 1.49 ug/mL, respectively.
Molecular Weight

405.32

Formula

C₁₉H₁₂F₅N₅

CAS No.

1782970-28-8

SMILES

FC(C1=CC=C(NC2=NC(N3C4=CC(F)=C(F)C=C4N=C3C)=CN=C2)C=C1)(F)F

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (308.40 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4672 mL 12.3359 mL 24.6719 mL
5 mM 0.4934 mL 2.4672 mL 4.9344 mL
10 mM 0.2467 mL 1.2336 mL 2.4672 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.13 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.13 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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PTC-028
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