N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid
10-Propargyl-10-deazaaminopterin
CAS: 146464-95-1
Molecular Formula: C23H23N7O5
N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid - Names and Identifiers
| Name | 10-Propargyl-10-deazaaminopterin |
| Synonyms | Pdx Pralatrexate Unii-A8Q8I19Q20 FOLOTYN PRALATREXATE 10-Propargyl-10-deazaaminopterin 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 L-Glutamic acid, N-(4-(1-((2,4-diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)- N-(4-{1-[(2,4-diaMinopteridin-6-yl)Methyl]but-3-yn-1-yl}benzoyl)-L-glutaMic acid |
| CAS | 146464-95-1 |
| InChI | InChI=1/C23H23N7O5/c1-2-3-14(10-15-11-26-20-18(27-15)19(24)29-23(25)30-20)12-4-6-13(7-5-12)21(33)28-16(22(34)35)8-9-17(31)32/h1,4-7,11,14,16H,3,8-10H2,(H,28,33)(H,31,32)(H,34,35)(H4,24,25,26,29,30)/t14?,16-/m0/s1 |
N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid - Physico-chemical Properties
| Molecular Formula | C23H23N7O5 |
| Molar Mass | 477.47 |
| Density | 1.471±0.06 g/cm3(Predicted) |
| Melting Point | 215 °C(dec.) |
| Water Solubility | Insoluble in water |
| Solubility | Soluble in DMSO (28 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ |
| Appearance | powder to crystal |
| Color | White to Light yellow |
| pKa | 3.53±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.703 |
| Use | An inhibitor of DHFR (dihydrofolate reductase) |
| In vitro study | Pralatrexate and bortezomib showed a wide range of concentration-and time-dependent inhibitory effects on T-type lymphoma cell lines. Pralatrexate and bortezomib in combination induce potent apoptosis and caspase activation. Pralatrexate significantly regulated expression of p27,NOXA,HH3, and RFC-1 by Western blot analysis. Pralatrexate improves cellular delivery via RFC-1 and has greater intracellular drug retention through enhanced polyglutamylated conjugate production. Pralatrexate is thought to exert its pharmacological effects primarily by inhibiting DHFR, with IC 50 in the picomolar range. Pralatrexate has superior intracellular transport through reduced folate carrier and enhanced intracellular accumulation of polyglutamic acid. Pralatrexate exhibits antitumor activity, which is superior to the activity of other antifolates. The enhanced activity of Pralatrexate relative to methotrexate (MTX) is due to its more rapid transport and speed of polyglutamation, the former being less important when the vector is saturated. |
| In vivo study | Pralatrexate treatment resulted in treatment-related toxicities in the MV522 mouse model, such as significant wasting before death in some animals, however, the remaining mice all lost weight by 35 days after dosing. |
N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid - Introduction
Pralatrexate is an antifolate drug with a structure similar to folic acid. It acts on some cell lines with an IC50 of less than 300 nM.
Last Update：2022-10-16 17:14:00
N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid - Reference Information
| introduction | pralexat (Pralatrexate), as a new anti-tumor drug, is the first drug to treat PTCL. It is reported in the literature that pratexa is a new type of targeted folic acid preparation, which can preferentially gather in cancer cells. It can treat recurrent and refractory PTCL alone. It can not only completely inhibit dihydrofolate reductase (DHFR), but also competitively Inhibit the polyglutamine effect of foloyl polyglutamyl synthetase, block the synthesis of thymine and other biomolecules that rely on single carbon transfer, and interfere with the synthesis of DNA, promote the death of tumor cells and achieve therapeutic effects. At present, foreign clinical experts have begun to use praltixab for the treatment of PTCL, but the domestic application is still in the clinical trial stage. |
| nursing | nursing before medication, and improving various examinations: routine examination of liver and kidney function, blood routine, blood sugar, urine sugar and B- ultrasound pancreas were normal before treatment. Vitamin supplementation: Patients should be supplemented with folic acid and vitamin B12 in advance before the first use of praltrexa. intravenous injection site nursing: establish a safe venous access, strictly follow the doctor's advice to select the appropriate part of the forearm to give peripheral venous indwelling needle puncture, before administration to confirm that the puncture is successful, the blood return is good, the infusion is unobstructed. Praltrexa injection is accurately aspirated at the required dose according to the doctor's advice before administration, and the administration nurse is injected intravenously at a slow speed within 3 min. Before and after administration, the injection tube is connected with intravenous drip of normal saline for flushing to reduce the stimulation of drugs on blood vessels. |
| Biological activity | Pralatrexate is an antifolic acid drug with a structure similar to folic acid. It acts on some cell lines and has an IC50 lower than 300 nM. Pralatrexate can induce apoptosis of tumor cells. |
| Target | Value |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 02:00:07
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