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Catalog No.
Hypoxia-activated prodrug,inhibits H460/HT29 cell growth
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10mM (in 1mL DMSO)
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In stock
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TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug of bromo-isophosphoramide mustard [1].
Hypoxia is a prevailing feature of tumors due to the abnormal aspects and structure of tumor vasculatures. It is found that hypoxic tumors usually show resistance to the traditional chemo- and radiation therapies and hypoxic tumors are more metastatic and invasive. Since the hypoxic tumors are not hyperproliferative, the traditional anti-proliferation drugs are not suitable. As a hypoxia-activated prodrug, TH-302 can release the cytotoxic agent Br-IPM and selectively deliver it the to the tumor cells under the anoxic condition [1 and 2].
The activity of TH-302 is dependent on the degree of anoxia and the exposure time of the drug under hypoxia. Higher activity requires lower oxygen concentration. Different with tirapazamine (another HAP), TH-302 needed much severer hypoxia (about 0.1%) to keep high potency. When treated in a panel of 32 kinds of tumor cells, TH-302 showed modest cytotoxicity with IC50 values all above 40 μM under the normal air condition. In contrast, TH-302 exerted elevated anti-tumor potency under the hypoxic condition. The IC50 values of it were in a range from 0.1 to 90 μM. Among these tumor cells, the non-small cell lung cancer H460 cells were most sensitive against TH-302 treatment with IC50 value of 0.1±0.03 μM. Besides that, TH-302 also showed potent efficacies in many other tumor cells, including Caki-1 (renal), SK-MEL-5 (melanoma), DU145 (prostate) and HCT116 (colon), with IC50 values of 0.4, 0.7, 0.7 and 0.8 μM, respectively [1].
In mice bearing H460 xenografts, administration of TH-302 at doses of 6.25 to 50 mg/kg dose-dependently caused tumor growth inhibition (TGI) with 43% to 89% and 50 mg/kg TH-302 administration showed no hematologic toxicity. Apart from this, TH-302 was found to induce DNA damage. TH-302 at dose of 100 mg/kg for 6 hours resulted in notable increase of γH2AX-positive cells [2].
[1] Meng F, Evans J W, Bhupathi D, et al. Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302. Molecular cancer therapeutics, 2012, 11(3): 740-751.
[2] Sun J D, Liu Q, Wang J, et al. Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer. Clinical cancer research, 2012, 18(3): 758-770.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.918633-87-1
SynonymsTH 302,TH302,HAP-302,HAP302
Solubility≥22.45 mg/mL in DMSO; ≥34.2 mg/mL in EtOH with ultrasonic; ≥4.73 mg/mL in H2O with gentle warming and ultrasonic
Chemical Name2-bromo-N-[(2-bromoethylamino)-[(3-methyl-2-nitroimidazol-4-yl)methoxy]phosphoryl]ethanamine
SDFDownload SDF
Canonical SMILESCN1C(=CN=C1[N+](=O)[O-])COP(=O)(NCCBr)NCCBr
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description TH-302 is a hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM).
Targets thioredoxin reductase glutathione reductase        

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