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PTC-028

PTC-028
PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.
Catalog No. T16680Cas No. 1782970-28-8
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Purity:97.61%
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PTC-028

Catalog No. T16680Cas No. 1782970-28-8

PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.
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Pack SizePriceAvailabilityQuantity
2 mg$32In Stock
5 mg$53In Stock
10 mg$88In Stock
25 mg$178In Stock
50 mg$296In Stock
100 mg$433In Stock
200 mg$616In Stock
1 mL x 10 mM (in DMSO)$65In Stock
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Product Introduction

Bioactivity
Description
PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.
In vitro
PTC-028 subsequently decreases BMI-1 in the biochemical functional readout. PTC-028 (100 nM; 2-12 hours) increases the phosphorylated BMI-1 species in a time-dependent manner. uH2A is observed up to 12 h with PTC-028 (100 nM) in both CP20 and OV90 cells while total H2A levels remain unchanged. PTC-028 (100 nM; 48 hours) decreases the expression of XIAP and RIPK1 while LC3B levels remain unchanged compared to that of the control. PTC-028 (25-500 nM; 48 hours) obviously reduces CP20, OVCAR4, and OV90 epithelial ovarian cancer cell 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 a minimal effect (~18-30% decrease). Significant cleavage of Caspase 7, Caspase 9, and PARP is observed in PTC-028 (100 nM; 48 hours)[1].
In vivo
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 decrease. PTC-028 (15 mg/kg; administered orally twice weekly) induces ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].
Chemical Properties
Molecular Weight405.32
FormulaC19H12F5N5
Cas No.1782970-28-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (308.40 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4672 mL12.3359 mL24.6719 mL123.3593 mL
5 mM0.4934 mL2.4672 mL4.9344 mL24.6719 mL
10 mM0.2467 mL1.2336 mL2.4672 mL12.3359 mL
20 mM0.1234 mL0.6168 mL1.2336 mL6.1680 mL
50 mM0.0493 mL0.2467 mL0.4934 mL2.4672 mL
100 mM0.0247 mL0.1234 mL0.2467 mL1.2336 mL

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