A hypoxia-activated prodrug and DNA alkylating agent with anticancer activity; selectively cytotoxic to H460 human NSCLC cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM

TH-302 – 1 mg

Brand:
Cayman
CAS:
918633-87-1
Storage:
-20
UN-No:
Non-Hazardous - /

TH-302 is a hypoxia-activated prodrug and DNA alkylating agent with anticancer activity.{43360} 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).{43360} 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.{43361}  

 

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Description

A hypoxia-activated prodrug and DNA alkylating agent with anticancer activity; selectively cytotoxic to H460 human NSCLC cells grown under hypoxic over normoxic conditions (IC50s = 0.019 and 5.1 μM, respectively); reduces survival of H460 and HT-29 cells in a clonogenic assay (IC50s = 0.2 and 0.2 μM, respectively); inhibits primary tumor growth by 41% in an MIA PaCa-2-RFP mouse orthotopic xenograft model at 33 mg/kg per day; inhibits tumor growth in the Calu-6 NSCLC, H82 small cell lung, A375 melanoma, PC-3 prostate, and BxPC-3 pancreatic cancer mouse xenograft models at 50 mg/kg

Formal name: N,N’-bis(2-bromoethyl)-phosphorodiamidic acid, (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester

Synonyms:  Evofosfamide

Molecular weight: 449

CAS: 918633-87-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|DNA Alkylating Agents||Research Area|Cancer|Cell Death||Research Area|Cancer|DNA Damage and Repair|DNA Alkylating Agents||Research Area|Cancer|Tumor Microenvironment

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