PTC-028|cas:1782970-28-8|西域试剂

PTC-028,98.0%

产品编号：Bellancom-103696| CAS NO：1782970-28-8| 分子式：C₁₉H₁₂F₅N₅| 分子量：405.32

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货号	价格	库存与货期
Bellancom-103696	￥950.00	杭州北京（现货）
Bellancom-103696	￥1500.00	杭州北京（现货）
Bellancom-103696	￥3050.00	杭州北京（现货）
Bellancom-103696	￥5100.00	杭州北京（现货）
Bellancom-103696	￥8000.00	杭州北京（现货）

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PTC-028

产品介绍

PTC-028 是一种口服有效的干细胞因子 BMI-1 的抑制剂，可用于研究卵巢癌。PTC-028 选择性地抑制癌细胞，而正常细胞不受影响。PTC-028 可下调 BMI-1，诱导 caspase 介导的细胞凋亡 (apoptosis)。

生物活性

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. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis.

体外研究

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).
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 .
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 remains unchanged compared to that of the control .
Significant cleavage of Caspase 7, Caspase 9 and PARP is observed in PTC-028 (100 nM; 48 hours).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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.

体内研究
(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) .
No obvious toxicity is noted in the animals during therapy experiments as assessed by mean body weight.
PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The C_max is reached at both dose levels 1h post dose after which plasma concentrations slowly reduce.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice with implanted OV90 cells
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
Dosage:	10 mg/kg or 20mg/kg
Administration:	Oral administered; single dose
Result:	Total plasma AUC_0-24h were 10.9 and 26.1 μg•h/mL at doses of 10 and 20 mg/kg. The C_max for PTC-028 at 10 and 20 mg/kg was 0.79 and 1.49 ug/mL, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice with implanted OV90 cells
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
Dosage:	10 mg/kg or 20mg/kg
Administration:	Oral administered; single dose
Result:	Total plasma AUC_0-24h were 10.9 and 26.1 μg•h/mL at doses of 10 and 20 mg/kg. The C_max for PTC-028 at 10 and 20 mg/kg was 0.79 and 1.49 ug/mL, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice with implanted OV90 cells
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
Dosage:	10 mg/kg or 20mg/kg
Administration:	Oral administered; single dose
Result:	Total plasma AUC_0-24h were 10.9 and 26.1 μg•h/mL at doses of 10 and 20 mg/kg. The C_max for PTC-028 at 10 and 20 mg/kg was 0.79 and 1.49 ug/mL, respectively.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

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

此方案可获得 ≥ 2.08 mg/mL (5.13 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
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

此方案可获得 ≥ 2.08 mg/mL (5.13 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。