AZD3965
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- CAS-Nr.
- 1448671-31-5
- Englisch Name:
- AZD3965
- Synonyma:
- CS-2201;AZD-3965;AZD3965;AZD 3965;AZD3965,inhibit,Inhibitor,Monocarboxylate Transporter;(S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;5-{[(4S)-4-Hydroxy-4-methyl-1,2-oxazolidin-2-yl]carbonyl}-1-isopropyl-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;5-[[(4S)-4-Hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione;Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-
- CBNumber:
- CB63034312
- Summenformel:
- C21H24F3N5O5S
- Molgewicht:
- 515.51
- MOL-Datei:
- 1448671-31-5.mol
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AZD3965 Eigenschaften
- Siedepunkt:
- 723.1±70.0 °C(Predicted)
- Dichte
- 1.483±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- L?slichkeit
- insoluble in H2O; ≥51.5 mg/mL in DMSO; ≥51.6 mg/mL in EtOH
- Aggregatzustand
- A crystalline solid
- pka
- 10.92±0.50(Predicted)
- Farbe
- White to off-white
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H320 |
Causes eye irritation |
Serious eye damage/eye irritation |
Category 2B |
Warnung |
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P264, P305+P351+P338,P337+P313 |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P337+P313 |
Bei anhaltender Augenreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
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AZD3965 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; K
i = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport. It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 μM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts. AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.
Enzyminhibitor
This orally bioavailable MCT1 inhibitor (FW = 515.51 g/mol; CASs =
733809-45-5 and 1448671-31-5), also named (S) -5- (4-hydroxy-4-
methylisoxazolidine-2-carbonyl) -1-isopropyl-3-methyl-6- ( (3-methyl-5- (tri-
fluoromethyl) -1H-pyrazol-4-yl) methyl) -thieno[2,3-d]pyrimidine-2,4 (1H,
3H) -dione, selectively targets the Monocarboxylate Transporter-1 (IC50 =
1.6 nM) and is ~6x less active toward MCT2. AZD3965 does not inhibit
MCT4, even at 10 μM. MCT1 and MCT4 are primarily involved in lactate
transport, targeting highly glycolytic cancer cells, especially those that are
hypoxic. The latter property suggests that the combined use with a
vascular-disrupting anticancer agent (such as combrestatin) may improve
the inhibitory action of AZD-3965 against cancer cells.
AZD3965 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
AZD3965 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 77)Lieferanten
- 5-[[(4S)-4-Hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- (S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- CS-2201
- AZD-3965;AZD3965;AZD 3965
- 5-{[(4S)-4-Hydroxy-4-methyl-1,2-oxazolidin-2-yl]carbonyl}-1-isopropyl-3-methyl-6-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl}thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
- Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-
- AZD3965,inhibit,Inhibitor,Monocarboxylate Transporter
- 1448671-31-5
