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Pralatrexate

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Chemical Structure| 146464-95-1 同义名 : NSC 754230;10-Propargyl-10-deazaaminopterin;PDX
CAS号 : 146464-95-1
货号 : A243480
分子式 : C23H23N7O5
纯度 : 99%+
分子量 : 477.473
MDL号 : MFCD00920897
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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
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 - -
实验方案
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
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