CAS 146464-95-1|Pralatrexate

Introduction：Basic information about CAS 146464-95-1|Pralatrexate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Pralatrexate BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	Pralatrexate
CAS Number	146464-95-1	Molecular Weight	477.473
Density	1.5±0.1 g/cm3	Boiling Point	/
Molecular Formula	C₂₃H₂₃N₇O₅	Melting Point	215 °C(dec.)
MSDS	/	Flash Point	/

Names

Name	pralatrexate
Synonym	More Synonyms

Pralatrexate BiologicalActivity

Description	Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.IC50 Value: < 300 nMTarget: AntifolatePralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. Based on preclinical studies, researchers believe that Pralatrexate selectively enters cells expressing reduced folate carrier type 1 (RFC-1), a protein that is overexpressed on certain cancer cells compared to normal cells.
Related Catalog	Signaling Pathways >>Cell Cycle/DNA Damage >>AntifolateResearch Areas >>Cancer
References	[1]. Foss F, Horwitz SM, Coiffier B, Bartlett N, Popplewell L, Pro B, Pinter-Brown LC, Shustov A, Furman RR, Haioun C, Koutsoukos T, O'Connor OA.,Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study,Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. Epub 2012 Apr 26. [2]. 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. [3]. Horwitz SM, Kim YH, Foss F, Zain JM, Myskowski PL, Lechowicz MJ, Fisher DC, Shustov AR, Bartlett NL, Delioukina ML, Koutsoukos T, Saunders ME, O'Connor OA, Duvic M.,Identification of an active, well-tolerated dose of pralatrexate in patients with relapsed or refractory cutaneous T-cell lymphoma.,Blood. 2012 May 3;119(18):4115-22. Epub 2012 Mar 6. [4]. Casanova M, Medina-Pérez A, Moreno-Beltran M, Mata-Vazquez M, Rueda A.,Critical appraisal of pralatrexate in the management of difficult-to-treat peripheral T cell lymphoma.,Ther Clin Risk Manag. 2011;7:401-8. Epub 2011 Oct 7. [5]. Hui J, Przespo E, Elefante A.,Pralatrexate: a novel synthetic antifolate for relapsed or refractory peripheral T-cell lymphoma and other potential uses.,J Oncol Pharm Pract. 2012 Jun;18(2):275-83. Epub 2011 Sep 26.

Description

Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.IC50 Value: < 300 nMTarget: AntifolatePralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. Based on preclinical studies, researchers believe that Pralatrexate selectively enters cells expressing reduced folate carrier type 1 (RFC-1), a protein that is overexpressed on certain cancer cells compared to normal cells.

Related Catalog

Signaling Pathways >>Cell Cycle/DNA Damage >>AntifolateResearch Areas >>Cancer

References

[1]. Foss F, Horwitz SM, Coiffier B, Bartlett N, Popplewell L, Pro B, Pinter-Brown LC, Shustov A, Furman RR, Haioun C, Koutsoukos T, O'Connor OA.,Pralatrexate Is an Effective Treatment for Relapsed or Refractory Transformed Mycosis Fungoides: A Subgroup Efficacy Analysis From the PROPEL Study,Clin Lymphoma Myeloma Leuk. 2012 Aug;12(4):238-43. Epub 2012 Apr 26.

[2]. 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.

[3]. Horwitz SM, Kim YH, Foss F, Zain JM, Myskowski PL, Lechowicz MJ, Fisher DC, Shustov AR, Bartlett NL, Delioukina ML, Koutsoukos T, Saunders ME, O'Connor OA, Duvic M.,Identification of an active, well-tolerated dose of pralatrexate in patients with relapsed or refractory cutaneous T-cell lymphoma.,Blood. 2012 May 3;119(18):4115-22. Epub 2012 Mar 6.

[4]. Casanova M, Medina-Pérez A, Moreno-Beltran M, Mata-Vazquez M, Rueda A.,Critical appraisal of pralatrexate in the management of difficult-to-treat peripheral T cell lymphoma.,Ther Clin Risk Manag. 2011;7:401-8. Epub 2011 Oct 7.

[5]. Hui J, Przespo E, Elefante A.,Pralatrexate: a novel synthetic antifolate for relapsed or refractory peripheral T-cell lymphoma and other potential uses.,J Oncol Pharm Pract. 2012 Jun;18(2):275-83. Epub 2011 Sep 26.

Chemical & Physical Properties

Density	1.5±0.1 g/cm3
Melting Point	215 °C(dec.)
Molecular Formula	C₂₃H₂₃N₇O₅
Molecular Weight	477.473
Exact Mass	477.176056
PSA	207.30000
LogP	0.23
Index of Refraction	1.704
InChIKey	OGSBUKJUDHAQEA-WMCAAGNKSA-N
SMILES	C#CCC(Cc1cnc2nc(N)nc(N)c2n1)c1ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc1

Safety Information

Hazard Codes	Xi

Synonyms

pralatrexato

pralatrexatum

10-Propargyl-10-deazaaminopterin

N-{4-[1-(2,4-Diamino-6-pteridinyl)-4-pentyn-2-yl]benzoyl}-L-glutamic acid

Folotyn

N-{4-[1-(2,4-Diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl}-L-glutamic acid

N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid

(2S)-2-[[4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl]amino]pentanedioic acid

L-Glutamic acid, N-[4-[1-[(2,4-diamino-6-pteridinyl)methyl]-3-butyn-1-yl]benzoyl]-

Pralatrexate

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