| Identification | Back Directory | [Name]
N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester | [CAS]
918633-87-1 | [Synonyms]
TH 302
CS-516
EOS-61724
EVOFOSFAMID
EvofosfaMide
TH-302, >=98%
TH 302; TH302
Evofosfamide(TH 302)
TH-302 (Evofosfamide)
(1-methyl-2-nitro-1H-imidazol-5-yl)methylN,N'-bis(2-bromoethyl)diamidophosphate
(1-Methyl-2-nitro-1H-imidazol-5-yl)methyl N,N'-bis(2-bromoethyl)phosphorodiamidate
N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester
2-bromo-N-[(2-bromoethylamino)-[(3-methyl-2-nitroimidazol-4-yl)methoxy]phosphoryl]ethanamine
Phosphorodiamidic acid, N,N'-bis(2-bromoethyl)-, (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester | [Molecular Formula]
C9H16Br2N5O4P | [MDL Number]
MFCD22420822 | [MOL File]
918633-87-1.mol | [Molecular Weight]
449.04 |
| Chemical Properties | Back Directory | [Melting point ]
97-98°C | [Boiling point ]
565.4±60.0 °C(Predicted) | [density ]
1.97 | [storage temp. ]
Hygroscopic, -20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
0.34±0.70(Predicted) | [color ]
Off-White to Pale Yellow |
| Hazard Information | Back Directory | [Description]
TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity.1 It is selectively cytotoxic to H460 human non-small cell lung cancer (NSCLC) cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM, respectively).1 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 (IC50s = 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.2 | [Uses]
TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-isophosphoramide mustard. Studies have shown that TH-302 treatment exhibited hypoxia-selective cytotoxicity and DNA dama
ge in human cancer cell | [storage]
Store at -20°C |
|
| Company Name: |
China Langchem Inc.
|
| Tel: |
0086-21-58956006 |
| Website: |
www.is0513.com/ShowSupplierProductsList19141/0.htm |
|