918633-87-1 Usage
Description
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 (IC50s = 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 (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.
Uses
Different sources of media describe the Uses of 918633-87-1 differently. You can refer to the following data:
1. 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
2. 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 damage in human cancer cell
Check Digit Verification of cas no
The CAS Registry Mumber 918633-87-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,8,6,3 and 3 respectively; the second part has 2 digits, 8 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 918633-87:
(8*9)+(7*1)+(6*8)+(5*6)+(4*3)+(3*3)+(2*8)+(1*7)=201
201 % 10 = 1
So 918633-87-1 is a valid CAS Registry Number.
918633-87-1Relevant articles and documents
Preparation method of evofosfamide
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, (2020/02/20)
The invention relates to a synthetic method for preparing evofosfamide, namely N,N'-bis(2-bromoethyl)diaminophosphonic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester (I), and belongs to the field of organic synthesis. The synthetic method has the advantages of safe and stable route, convenient operation, easy purification, high yield and the like.
TH-302 SOLID FORMS AND METHODS RELATED THERETO
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, (2016/02/10)
The present invention provides a new method for making TH-302 and solid forms thereof. The compound in its solid form is an effective anti-cancer agent and may be used in various pharmaceutical compositions, and are particularly effective for the treatment of cancer. The invention also provides a method for preparing such compounds and forms and for treating cancer in a mammal comprising the step of administering a therapeutically effective amount of a solid form of TH-302 thereof.
PHOSPHORAMIDATE ALKYLATOR PRODRUGS
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Page/Page column 125-126, (2008/06/13)
Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
