Lometrexol
|
|
|
- CAS-Nr.
- 106400-81-1
- Englisch Name:
- Lometrexol
- Synonyma:
- LY 264618;Lometrexol;Lometrexolum;LY 264618 hydrate;Lometrexol hydrate;Lometrexol(LY 264618);Lometrexolum [inn-latin];(6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid;N-[4-[2-[[(R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid;L-Glutamic acid, N-(4-(2-((6R)-2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-
- CBNumber:
- CB81179064
- Summenformel:
- C21H25N5O6
- Molgewicht:
- 443.45
- MOL-Datei:
- 106400-81-1.mol
|
Lometrexol Eigenschaften
- Dichte
- 1.56±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- DMSO: ≥5mg/mL
- pka
- 3.60±0.10(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to light yellow
- Stabilit?t:
- Hygroscopic
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Kennzeichnung gef?hrlicher |
T |
|
|
| R-S?tze: |
25 |
|
|
| S-S?tze: |
45 |
|
|
| RIDADR |
UN 2811 6.1 / PGIII |
|
|
| WGK Germany |
3 |
|
|
| Bildanzeige (GHS) |
|
| Alarmwort |
Achtung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H301 |
Giftig bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 3 |
Achtung |
![GHS hazard pictograms]() src="/GHS06.jpg" width="20" height="20" /> |
P264, P270, P301+P310, P321, P330,P405, P501 |
|
| Sicherheit |
| P301+P310 |
BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
|
Lometrexol Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Glycinamide ribonucleotide formyltransferase (GART) is a folate-dependent enzyme required for
de novo purine synthesis. Lometrexol is a folate analog antimetabolite with antineoplastic activity. At nanomolar conentrations, it inhibits GART preventing
de novo purine synthesis, inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation.
Verwenden
Lometrexol hydrate was used to compare the biological activity of potent inhibitor of human GARFTase.
Biochem/physiol Actions
Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.
Lometrexol Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Lometrexol Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 28)Lieferanten
106400-81-1()Verwandte Suche:
- Lometrexol
- (6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid
- N-[4-[2-[[(6R)-2-Amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid
- N-[4-[2-[[(R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid
- L-Glutamic acid, N-(4-(2-((6R)-2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-
- L-Glutamic acid, N-(4-(2-(2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-, (R)-
- Lometrexolum
- Lometrexolum [inn-latin]
- LY 264618
- Lometrexol hydrate
- LY 264618 hydrate
- N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid hydrate
- Lometrexol(LY 264618)
- L-Glutamic acid, N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-
- 106400-81-1
- Aromatics
- Chiral Reagents
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
