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10-Propargyl-10-deazaaminopterin

10-Propargyl-10-deazaaminopterin Struktur
146464-95-1
CAS-Nr.
146464-95-1
Englisch Name:
10-Propargyl-10-deazaaminopterin
Synonyma:
Pralatrexate;Pdx;Folotyn;CS-2172;Pralatrexat;Prelatrexate;Unii-A8Q8I19Q20;Pralatrexate, >=98%;FOLOTYN PRALATREXATE;Pralatrexate(Folotyn)
CBNumber:
CB31856065
Summenformel:
C23H23N7O5
Molgewicht:
477.47
MOL-Datei:
146464-95-1.mol

10-Propargyl-10-deazaaminopterin Eigenschaften

Schmelzpunkt:
215 °C(dec.)
Dichte
1.471±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
Wasserl?slichkeit
Insoluble in water
L?slichkeit
≥23.85 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
pka
3.53±0.10(Predicted)
Aggregatzustand
powder to crystal
Farbe
White to Light yellow
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
HS Code  2933.59.5300
Giftige Stoffe Daten 146464-95-1(Hazardous Substances Data)
Bildanzeige (GHS) GHS hazard pictogramsGHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H361 Kann vermutlich die Fruchtbarkeit beeintr?chtigen oder das Kind im Mutterleib sch?digen. Reproduktionstoxizit?t Kategorie 2 Warnung P201, P202, P281, P308+P313, P405,P501
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P202 Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P270 Bei Gebrauch nicht essen, trinken oder rauchen.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P308+P313 BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.
P405 Unter Verschluss aufbewahren.
P501 Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

10-Propargyl-10-deazaaminopterin Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Pralatrexate, an injectable DHFR inhibitor, was launched for the treatment of patients with relapsed or refractory PTCL. PTCL is an aggressive form of non-Hodgkin’s lymphoma (NHL) characterized by the proliferation of abnormal T-lymphocytes that circulate in the peripheral bloodstream. The inhibition of the folate enzymes DHFR and thymidylate synthase is a well-validated method of cancer treatment. In vitro, pralatrexate is slightly less potent than MTX in inhibiting DHFR derived from murine leukemia L1210 cells (Ki = 18.2 pM vs. 5.75 pM) and human leukemia CCRF-CEM cells (Ki = 13.4 pM vs. 5.4 pM). However, it is transported into both types of cells with 10-fold higher efficiency than MTX, thereby providing a more potent inhibition of cell growth as compared with MTX. In vivo, intraperitonally administered pralatrexate at 60 mg/ kg twice weekly for three or four doses caused complete lymphoma regressions in 89, 56, and 30% of HT, RL, and SKI-DLBCL-1 xenografted mice, respectively, whereas a similar dosing of MTX at 40 mg/kg twice weekly did not produce complete regression. The posttreatment tumor diameter was also smaller in pralatrexate-treated animals.

Verwenden

An antifolate with high affinity for the reduced folate carrier-type 1, produces marked complete and durable remissions in a diversity of chemotherapy refractory cases of T-cell lymphoma.

Definition

ChEBI: A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.

Clinical Use

Pralatrexate, an injectable dihydrofolate reductase (DHFR) inhibitor, has a superior potency and toxicity profile compared to other DHFR inhibitors. In 2009, the compound was launched by Allos and approved in the U.S. for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL) as a single agent. It is the first drug approved for this indication.70 In 2010, orphan drug designation was received in the E.U. for the treatment of cutaneous T-cell lymphoma (CTCL).

Nebenwirkungen

The most common adverse reactions associated with pralatrexate are mucositis, thrombocytopenia, nausea, and fatigue. Folic acid and vitamin B12 supplements are administered as adjunct therapies to potentially reduce pralatrexate-related hematological toxicity and mucositis.

10-Propargyl-10-deazaaminopterin Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


10-Propargyl-10-deazaaminopterin Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 174)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
+86-18600796368 +86-18600796368
sales@sjar-tech.com China 456 58
Shanghai Daken Advanced Materials Co.,Ltd
+86-371-66670886
info@dakenam.com China 18751 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55
Hangzhou FandaChem Co.,Ltd.
+8615858145714
FandaChem@Gmail.com China 9087 55
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 295 58
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28172 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58

146464-95-1()Verwandte Suche:


  • N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid
  • 10-Propargyl-10-deazaaminopterin
  • L-Glutamic acid, N-(4-(1-((2,4-diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-
  • Unii-A8Q8I19Q20
  • FOLOTYN PRALATREXATE
  • N-(4-{1-[(2,4-diaMinopteridin-6-yl)Methyl]but-3-yn-1-yl}benzoyl)-L-glutaMic acid
  • N-[4-[1-[(2,4-DiaMino-6-pteridinyl)Methyl]-3-butyn-1-yl]benzoyl]-L-glutaMic Acid
  • (2S)-2-(4-(1-(2,4-diaMinopteridin-6-yl)pent-4-yn-2-yl)benzaMido)pentanedioic acid
  • Prelatrexate
  • 10-Propargyl-10-deazaaMinopteri
  • Pralatrexate(Folotyn)
  • 10-Propargyl-10-deazaaminopterin N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid
  • N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid Pralatrexate
  • Pralatrexate, >=98%
  • Pralatrexat
  • CS-2172
  • Pralatrexate Impurity
  • L-Glutamic acid, N-[4-[1-[(2,4-diamino-6-pteridinyl)methyl]-3-butyn-1-yl]benzoyl]-
  • 10-Propargyl-10-deazaaminopterin USP/EP/BP
  • Pralatrexate (racemic)
  • Pralatrexate
  • Pdx
  • Folotyn
  • 146464-95-1 10-Propargyl-10-deazaaminopterin
  • Pralatrexate (NSC 754230)
  • 146464-95-1
  • Amino Acids & Derivatives
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
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