1. Apoptosis
  2. Apoptosis
  3. PTC-028

PTC-028 

目录号: HY-103696
产品使用指南

PTC-028 是一种口服有效的干细胞因子 BMI-1 的抑制剂,可用于治疗卵巢癌。PTC-028 选择性地抑制癌细胞,而正常细胞不受影响。PTC-028 对 BMI-1 的作用可诱导 caspase 介导的细胞凋亡 (apoptosis)。

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PTC-028 Chemical Structure

PTC-028 Chemical Structure

CAS No. : 1782970-28-8

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10 mM * 1 mL in DMSO ¥1210 In-stock
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50 mg ¥6100 In-stock
100 mg ¥9600 In-stock
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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 in 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 remained unchanged [1].
PTC-028 (100 nM; 48 hours) significantly decreases BMI-1. However, PTC-028 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 poly ADP-ribose polymerase (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) caused ~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.
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
*请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液。
In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂
(以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

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

*以上所有助溶剂都可在 MCE 网站选购。
References
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

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产品名称:
PTC-028
目录号:
HY-103696
需求量:

PTC-028

Cat. No.: HY-103696