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首页 / 抑制剂/激动剂 / 细胞周期 / DHFR / Pralatrexate

普拉曲沙 /Pralatrexate {[allProObj[0].p_purity_real_show]}

货号：A243480 同义名： NSC 754230;10-Propargyl-10-deazaaminopterin

Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.

Pralatrexate 化学结构 CAS号：146464-95-1
Pralatrexate 化学结构
CAS号：146464-95-1
Pralatrexate 3D分子结构
CAS号：146464-95-1
Pralatrexate 化学结构 CAS号：146464-95-1
Pralatrexate 3D分子结构 CAS号：146464-95-1
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Pralatrexate 纯度/质量文件 产品仅供科研

货号：A243480 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 DHFR ↓ 其他靶点 纯度
Pralatrexate ✔ 99%+
Pemetrexed disodium ++++

DHFR, Ki: 7.2 nM

 		99.9%
Pyrimethamine ++

DHFR, IC50: 15.4 nM

 		98% HPLC
Pemetrexed ++++

DHFR , Ki: 7.2 nM

 		99+%
Methotrexate +

hDHFR, IC50: 24 nM

 		99% (contain ~10%water)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Pralatrexate 生物活性

靶点

  • DHFR
描述 Pralatrexate, a folate analogue targeting dihydrofolate reductase, has antitumor activity in non-small-cell lung cancer (NSCLC) [3]. Pralatrexate (10-propargyl-10-deazaaminopterin) is an antifolate with improved cellular uptake and retention due to greater affinity for the reduced folate carrier (RFC-1) and folyl-polyglutamyl synthase. In vitro, pralatrexate and bortezomib exhibited concentration- and time-dependent cytotoxicity against a broad panel of T-lymphoma cell lines[4]. Coadministration of pralatrexate and romidepsin was safe, well tolerated, with 3 DLTs across all schedules (grade 3 oral mucositis × 2; grade 4 sepsis × 1) [5].

Pralatrexate 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
Chinese hamster R2 cells Growth inhibition assay 96 h Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay, IC50=0.057 μM 24111942
human KB cells Growth inhibition assay 96 h Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay, IC50=0.47 nM 24111942

Pralatrexate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01626664 Adult T-cell Leukemia-Lymphoma Phase 2 Completed - United States, California ... 展开 >> Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 United States, Florida University of Miami / Sylvester Comprehensive Cancer Center Miami, Florida, United States, 33136 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Maryland National Cancer Institute Bethesda, Maryland, United States, 20892 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, New Jersey Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, New York Montefiore Medical Center Bronx, New York, United States, 10467 Memorial Sloan Kettering New York, New York, United States, 10021 Columbia Presbyterian New York, New York, United States, 10032 Weill Cornell Medical College New York, New York, United States, 10065 Belgium Cliniques Universitaires Saint-Luc Bruxelles, Belgium, 1200 Brazil Hospital Universitario Professor Edgard Santos- UFBA Salvador, Bahia, Brazil, 40110-060 Hospital das Clínicas da Faculdade de Medicina da Universidade de São Paulo Sao Paulo- SP, Brazil, CEP 05403-000 France CHU de Fort de France Fort De France Cedex, France, BP 632 97261 Hospital Necker Paris, France, 75743 Peru Hospital Nacional Edgardo Rebagliati Martins Lima, Peru, Lima11 Instituto Oncologico Miraflores Lima, Peru, Lima18 United Kingdom Guy's Hospital London, United Kingdom, SE1 9RT Imperial College London, United Kingdom, W2 1PG Sandwell General Hospital West Midlands, United Kingdom, B71 4HJ 收起 <<
NCT01626664 - Completed - -
NCT01482962 - Completed - -

Pralatrexate 参考文献

[1]Marchi E, Paoluzzi L, et al. Pralatrexate is synergistic with the proteasome inhibitor bortezomib in in vitro and in vivo models of T-cell lymphoid malignancies. Clin Cancer Res. 2010 Jul 15;16(14):3648-58.

[2]Izbicka E, Diaz A, et al. Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers. Cancer Chemother Pharmacol. 2009 Oct;64(5):993-9.

[3]Kelly K, Azzoli CG, Zatloukal P, Albert I, Jiang PY, Bodkin D, Pereira JR, Juhász E, Iannotti NO, Weems G, Koutsoukos T, Patel JD. Randomized phase 2b study of pralatrexate versus erlotinib in patients with stage IIIB/IV non-small-cell lung cancer (NSCLC) after failure of prior platinum-based therapy. J Thorac Oncol. 2012 Jun;7(6):1041-8

[4]Marchi E, Paoluzzi L, Scotto L, Seshan VE, Zain JM, Zinzani PL, O'Connor OA. Pralatrexate is synergistic with the proteasome inhibitor bortezomib in in vitro and in vivo models of T-cell lymphoid malignancies. Clin Cancer Res. 2010 Jul 15;16(14):3648-58

[5]Amengual JE, Lichtenstein R, Lue J, Sawas A, Deng C, Lichtenstein E, Khan K, Atkins L, Rada A, Kim HA, Chiuzan C, Kalac M, Marchi E, Falchi L, Francescone MA, Schwartz L, Cremers S, O'Connor OA. A phase 1 study of romidepsin and pralatrexate reveals marked activity in relapsed and refractory T-cell lymphoma. Blood. 2018 Jan 25;131(4):397-407

Pralatrexate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.94mL

4.19mL

2.09mL

Pralatrexate 技术信息

CAS号146464-95-1
分子式C23H23N7O5
分子量 477.473
别名 NSC 754230;10-Propargyl-10-deazaaminopterin;PDX
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 50 mg/mL(104.72 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Pralatrexate | NSC 754230;10-Propargyl-10-deazaaminopterin;PDX | DHFR | AmBeed-信号通路专用抑制剂 | Pralatrexate 纯度/质量文件 | Pralatrexate 亚型比较 | Pralatrexate 生物活性 | Pralatrexate 细胞研究 | Pralatrexate 临床数据 | Pralatrexate 参考文献 | Pralatrexate 实验方案 | Pralatrexate 技术信息

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