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PTC-028

Catalog No. T16680 CAS 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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PTC-028, CAS 1782970-28-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 493.00
100 mg	In stock	$ 723.00
500 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 109.00

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Purity: 98.25%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Molecular Weight	405.32
Formula	C19H12F5N5
CAS No.	1782970-28-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (308.40 mM), Sonification is recommended.

References and Literature

1. Dey A, et al. Evaluating the Mechanism and Therapeutic Potential of PTC-028, a Novel Inhibitor of BMI-1 Function in Ovarian Cancer. Mol Cancer Ther. 2018 Jan;17(1):39-49.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Preclinical Compound Library DNA Damage & Repair Compound Library Hematonosis Compound Library Ferroptosis Compound Library Anti-Aging Compound Library NO PAINS Compound Library Apoptosis Compound Library Bioactive Compounds Library Max

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Keywords

PTC-028 1782970-28-8 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair BMI-1 inhibit Inhibitor PTC 028 PTC028 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.