标签归档：ptc

Unesbulin(Synonyms: PTC596)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Unesbulin (Synonyms: PTC596) 纯度: 98.22%

Unesbulin (PTC596) 是一种口服有效和选择性的 B 细胞特异性莫洛尼氏鼠白血病病毒整合位点 1 (BMI-1) 抑制剂。Unesbulin 在急性髓细胞白血病 (AML) 细胞中可下调 MCL-1 并诱导不依赖 p53 的线粒体凋亡。Unesbulin 具有抗白血病作用。

Unesbulin(Synonyms: PTC596)

Unesbulin Chemical Structure

CAS No. : 1610964-64-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3237 In-stock
1 mg ￥1200 In-stock
5 mg ￥3000 In-stock
10 mg ￥4600 In-stock
25 mg ￥6800 In-stock
50 mg ￥9950 In-stock
100 mg 询价

* Please select Quantity before adding items.

Unesbulin 相关产品

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  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity[1][2].

IC50 & Target

BMI-1[1]
体外研究
(In Vitro)

Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis[1].
Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase[1].
Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1[1].
Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: AML cell lines (MOLM-13, OCI-AML3, MOLM-14, MV4-11, U-937, HL-60)
Concentration: 20, 50, 100, 200 nM
Incubation Time: For 48 hours
Result: Induced apoptosis in a dose- and time-dependent manner with the average IC50 and ED50 values among six cell lines were 30.7 nM and 60.3 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: MOLM-13 and U-937 cells
Concentration: 200 nM
Incubation Time: For 10 hours
Result: Led to an accumulation of cells in G2/M phase, whereas the percentage of cells in G1 phase decreased.

Western Blot Analysis[1]

Cell Line: MOLM-13 cell
Concentration: 0.012, 0.037, 0.11, 0.33, 1 μM
Incubation Time: For 20 hours
Result: Significantly reduced protein levels of BMI-1 and its downstream target ubiquitinated histone H2A.
Increased cyclin B1 and securin levels.

体内研究
(In Vivo)

Unesbulin (PTC596; 5 mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival[1].
Unesbulin (20 mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells[1].
Unesbulin (10 or 12.5  mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD-SCID/IL2Rγ-KO (NSG) mice with MOLM-13 cells[1]
Dosage: 5 mg/kg
Administration: Oral gavage; every 3 days for 13 days
Result: Significantly prolonged mouse survival compared with the vehicle-treated mice in a dose-dependent manner.

Clinical Trial

分子量

420.34

Formula

C19H13F5N6
CAS 号

1610964-64-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (39.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3790 mL 11.8951 mL 23.7903 mL
5 mM 0.4758 mL 2.3790 mL 4.7581 mL
10 mM 0.2379 mL 1.1895 mL 2.3790 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: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.97 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.97 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Nishida Y, et al. The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells. Blood Cancer J. 2017 Feb 17;7(2):e527.

    [2]. BMI1 inhibitor PTC596

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PTC299

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PTC299  纯度: 99.52%

PTC299 是 VEGFA mRNA 翻译的具有口服活性抑制剂，在转录后水平选择性地抑制 VEGF 蛋白的合成。PTC299 也是二氢乳酸盐脱氢酶 (DHODH) 的有效抑制剂。PTC299 良好的口服生物利用度，缺乏脱靶激酶抑制和骨髓抑制。PTC299 可用于血液系统恶性肿瘤的研究。

PTC299

PTC299 Chemical Structure

CAS No. : 1256565-36-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4180 In-stock
5 mg ￥3800 In-stock
10 mg ￥5700 In-stock
25 mg ￥10500 In-stock
50 mg ￥16400 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

PTC299 相关产品

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  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Ferroptosis Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Mitochondria-Targeted Compound Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies[1][2].

IC50 & Target

VEGF[2]
体外研究
(In Vitro)

PTC299 inhibits hypoxia-induced VEGFA protein production in HeLa cells with an EC50 of 1.64 ± 0.83 nM[1].
PTC299 is the most potent inhibitor with an IC50 of about 1 nM, over 10 to 1000-fold more potent than Brequinar, Vidofludimus or A 77-1726 in leukemia cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

467.34

Formula

C25H20Cl2N2O3
CAS 号

1256565-36-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (106.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1398 mL 10.6988 mL 21.3977 mL
5 mM 0.4280 mL 2.1398 mL 4.2795 mL
10 mM 0.2140 mL 1.0699 mL 2.1398 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: ≥ 0.83 mg/mL (1.78 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.78 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 8.3 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: ≥ 0.83 mg/mL (1.78 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (1.78 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 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cao L, et al. Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of DihydroorotateDehydrogenase with Favorable Pharmaceutical Properties. Mol Cancer Ther. 2019 Jan;18(1):3-16.

    [2]. Bender Ignacio RA, et al. Brief Report: A Phase 1b/Pharmacokinetic Trial of PTC299, a Novel PostTranscriptional VEGF Inhibitor, for AIDS-Related Kaposi’s Sarcoma: AIDS Malignancy Consortium Trial 059. J Acquir Immune Defic Syndr. 2016 May 1;72(1):52-7.

    [3]. Packer RJ, et al. Phase I and pharmacokinetic trial of PTC299 in pediatric patients with refractory or recurrent central nervous system tumors: a PBTC study. J Neurooncol. 2015;121(1):217-224.

    [4]. Zeng Z, et al, Targeting dihydroorotate dehydrogenase in acute myeloid leukemia. Haematologica. 2018 Sep;103(9):1415-1417.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PTC-209 hydrobromide

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PTC-209 hydrobromide 

PTC-209 hydrobromide 是一种特定的 BMI-1 抑制剂，在 HEK293T 细胞系中的 IC50 为 0.5 μM。PTC-209 hydrobromide 不可逆转地损害结直肠癌起始细胞 (CICs)。PTC-209 hydrobromide 显示有效的抗骨髓瘤活性并损害肿瘤微环境。

PTC-209 hydrobromide

PTC-209 hydrobromide Chemical Structure

CAS No. : 1217022-63-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PTC-209 hydrobromide 的其他形式现货产品:

PTC-209

生物活性

PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment[1][2].

IC50 & Target

IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)[1]
体外研究
(In Vitro)

PTC-209 (0.01-10 µM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
Concentration: 0.01-10 µM
Incubation Time: 24, 48, and 72 hour
Result: Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.

体内研究
(In Vivo)

PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)[1]
Dosage: 60 mg/kg body weight
Administration: Subcutaneously; once a day for 11 days
Result: Significantly reduced tumor volume.

分子量

576.10

Formula

C17H14Br3N5OS
CAS 号

1217022-63-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.

    [2]. Christian Mayr, et al. The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells. Oncotarget. 2016 Jan 5; 7(1): 745-758.

    [3]. Shahi MH, et al. BMI1 is expressed in canine osteosarcoma and contributes to cell growth and chemotherapy resistance. PLoS One. 2015 Jun 25;10(6):e0131006.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PTC-209

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PTC-209  纯度: 99.85%

PTC-209 是一种特定的 BMI-1 抑制剂，在 HEK293T 细胞系中的 IC50 为 0.5 μM。PTC-209 不可逆转地损害结直肠癌起始细胞 (CICs)。PTC-209 显示有效的抗骨髓瘤活性并损害肿瘤微环境。

PTC-209

PTC-209 Chemical Structure

CAS No. : 315704-66-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1125 In-stock
5 mg ￥1023 In-stock
10 mg ￥1500 In-stock
50 mg ￥4900 In-stock
100 mg ￥8400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PTC-209 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Covalent Screening Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment[1][2].

IC50 & Target

IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)[1]
体外研究
(In Vitro)

PTC-209 (0.01-10 µM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
Concentration: 0.01-10 µM
Incubation Time: 24, 48, and 72 hour
Result: Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.

体内研究
(In Vivo)

PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)[1]
Dosage: 60 mg/kg body weight
Administration: Subcutaneously; once a day for 11 days
Result: Significantly reduced tumor volume

分子量

495.19

Formula

C17H13Br2N5OS
CAS 号

315704-66-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 32 mg/mL (64.62 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0194 mL 10.0971 mL 20.1943 mL
5 mM 0.4039 mL 2.0194 mL 4.0389 mL
10 mM 0.2019 mL 1.0097 mL 2.0194 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: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.05 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.

    [2]. Sulaiman S, et al. PTC-209 Anti-Cancer Effects Involved the Inhibition of STAT3 Phosphorylation. Front Pharmacol. 2019;10:1199. Published 2019 Oct 21.

    [3]. Chen D, et al. Targeting BMI1+ Cancer Stem Cells Overcomes Chemoresistance and Inhibits Metastases in Squamous Cell Carcinoma. Cell Stem Cell. 2017 May 4;20(5):621-634.e6.

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PTC-028

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PTC-028  纯度: ≥98.0%

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 可下调 BMI-1, 诱导 caspase 介导的细胞凋亡 (apoptosis)。

PTC-028

PTC-028 Chemical Structure

CAS No. : 1782970-28-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1045 In-stock
5 mg ￥950 In-stock
10 mg ￥1500 In-stock
25 mg ￥3050 In-stock
50 mg ￥5100 In-stock
100 mg ￥8000 In-stock
200 mg   询价  
500 mg   询价  

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PTC-028 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Targeted Diversity Library

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[1].

IC50 & Target

BMI-1[1]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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) [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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

405.32

Formula

C19H12F5N5
CAS 号

1782970-28-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务