N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester
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- CAS-Nr.
- 918633-87-1
- Englisch Name:
- N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester
- Synonyma:
- TH 302;CS-516;HAP-302;EOS-61724;EVOFOSFAMID;EvofosfaMide;TH-302, >=98%;TH 302; TH302;Evofosfamide(TH 302);TH-302 (Evofosfamide)
- CBNumber:
- CB52604209
- Summenformel:
- C9H16Br2N5O4P
- Molgewicht:
- 449.04
- MOL-Datei:
- 918633-87-1.mol
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N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester Eigenschaften
- Schmelzpunkt:
- 97-98°C
- Siedepunkt:
- 565.4±60.0 °C(Predicted)
- Dichte
- 1.97
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- L?slichkeit
- DMSO (Slightly), Methanol (Slightly)
- pka
- 0.34±0.70(Predicted)
- Aggregatzustand
- Solid
- Farbe
- Off-White to Pale Yellow
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| 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 pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
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| Sicherheit |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
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N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity. It is selectively cytotoxic to H460 human non-small cell lung cancer (NSCLC) cells grown under hypoxic over normoxic conditions (IC
50s = 0.019 and 5.1 μM, respectively). Under hypoxic conditions, TH-302 undergoes a one-electron reduction to form an active radical intermediate that is then further reduced to form a DNA-intercalating hydroxylamine. Under normoxic conditions, the radical intermediate is quenched and induces reformation of the inactive nitroazole prodrug. TH-302 reduces survival of H460 and HT-29 cells in a clonogenic assay (IC
50s = 0.2 and 0.2 μM, respectively).
In vivo, TH-302 (33 mg/kg per day) inhibits primary tumor growth by 41% in an MIA PaCa-2-RFP mouse orthotopic xenograft model. It inhibits tumor growth by greater than 40% in Calu-6 NSCLC, H82 small cell lung, A375 melanoma, PC-3 prostate, and BxPC-3 pancreatic cancer mouse xenograft models when administered at 50 mg/kg.
N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 112)Lieferanten
918633-87-1()Verwandte Suche:
- N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester
- TH 302
- EvofosfaMide
- TH-302, >=98%
- TH-302 (Evofosfamide)
- (1-methyl-2-nitro-1H-imidazol-5-yl)methylN,N'-bis(2-bromoethyl)diamidophosphate
- EOS-61724
- Evofosfamide(TH 302)
- EVOFOSFAMID
- 2-bromo-N-[(2-bromoethylamino)-[(3-methyl-2-nitroimidazol-4-yl)methoxy]phosphoryl]ethanamine
- (1-Methyl-2-nitro-1H-imidazol-5-yl)methyl N,N'-bis(2-bromoethyl)phosphorodiamidate
- CS-516
- TH 302; TH302
- Phosphorodiamidic acid, N,N'-bis(2-bromoethyl)-, (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester
- HAP-302
- 918633-87-1
- C9H16Br2N5O4P
- TH-302
- APIs
- API
