A DHFR inhibitor (Ki = 13.4 pM) and antifolate; inhibits growth of acute lymphocytic leukemia cells (IC50 = 0.04 μM)

Pralatrexate – 50 mg

Brand:
Cayman
CAS:
146464-95-1
Storage:
-20
UN-No:
De Minimis - 3077 / 6.1|9

Pralatrexate is a dihydrofolate reductase (DHFR) inhibitor (Ki = 13.4 pM) and antifolate.{39422} It inhibits growth of CCRF-CEM acute lymphocytic leukemia cells (IC50 = 0.04 μM), MDA-468, SK-BR-3, and ZR-75-1 breast cancer cells (IC50s = 0.11, 0.28, and 0.26 μM, respectively), and SK-LC8 and SK-LC16 non-small cell lung cancer cells (NSCLC; IC50s = 0.42 and 0.11 μM, respectively). In vivo, pralatrexate increases median survival from 21 to 40 days when administered in 4 doses of 15 mg/kg over 11 days in an H9 T cell lymphoma mouse xenograft model.{39423} Pralatrexate is transported into cells via the reduced folate carrier (RFC) and undergoes polyglutamation by folylpolyglutamate synthetase (FPGS) to a greater extent than methotrexate (Item No. 13960) or pemetrexed (Item No. 14269).{39424,39425} Formulations containing pralatrexate have been used in the treatment of relapsed or refractory peripheral T cell lymphoma.  

 

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Description

A DHFR inhibitor (Ki = 13.4 pM) and antifolate; inhibits growth of acute lymphocytic leukemia cells (IC50 = 0.04 μM), MDA-468, SK-BR-3, and ZR-75-1 breast cancer cells (IC50s = 0.11, 0.28, and 0.26 μM, respectively), and SK-LC8 and SK-LC16 NSCLC cells (IC50s = 0.42 and 0.11 μM, respectively); increases median survival in vivo in an H9 T cell lymphoma mouse xenograft model

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

Synonyms:  10-Propargyl-10-deazaaminopterin|NSC 754230|PDX

Molecular weight: 477.5

CAS: 146464-95-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer

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