Free shipping on all orders over $ 500

TH-302 (Evofosfamide)

Cat. No. M2206
TH-302 (Evofosfamide) Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 63  USD70 In stock
5mg USD 117  USD130 In stock
10mg USD 157.5  USD175 In stock
50mg USD 441  USD490 In stock
100mg USD 675  USD750 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM). TH-302 inhibits H460 cells and HT29 cells with IC90 of 0.1 μM and 0.2 μM, respectively. TH-302 exhibits potent cytotoxicity to both human and murine MM cells with hypoxic selectivity and dose dependency, and induces G0/G1 cell-cycle arrest under hypoxic conditions. TH-302 treatment resulted in a reduction in the volume of the HF 48 hours after dosing and a corresponding increase in the necrotic fraction. TH-302 is currently in a phase II clinical trial for the treatment of soft tissue sarcoma.

Product Citations
Customer Product Validations & Biological Datas
Source Plos One (2017). Figure 6. TH-302
Method Apoptosis assay
Cell Lines lymphoma cells
Concentrations 50 μM
Incubation Time 24 h
Results After treatment with 50 μMTH-302 for 24 h under 21% O2, the percentages of apoptotic cells in all the cell types were not significantly different from those of the vehicle-treated cells, and there were negligible morphological abnormalities among the cells
Source Plos One (2017). Figure 5. TH-302
Method Drug sensitivity testing
Cell Lines lymphoma cells
Concentrations 1, 10, 100, or 1000 nM
Incubation Time 24 h
Results However, after treatment with 50 μMTH-302 for 24 h under 10% O2, there were no significant differences in the viability of any cells
Cell Experiment
Cell lines H460, H82, DU145, A375 and PC3 cells line
Preparation method In vitro cytotoxicity assay
Exponentially growing cells were seeded 24 hours before the addition of test compounds. After drug addition, the plates were incubated for 2 hours, or longer if indicated, under defined oxygen concentrations at 37°C in an anaerobic chamber (Bactron II), a hypoxia chamber (Hypoxystation), or a standard tissue-culture incubator. Using this method, cells equilibrated rapidly (<30 minutes) with the gas phase as shown by linearity of time course of cytotoxicity and use of dissolved oxygen probe (OxyLite, Oxford Optronics). Cells were cultured for 72 hours in complete medium after washing under normoxic conditions, and the viable cells were quantified using AlamarBlue. For DPI experiments, cells were pretreated with 100 μmol/L of DPI for 2 hours under air. Drug concentration resulting in growth inhibition of 50% (IC50) relative to untreated control was calculated using Prism software.
Concentrations 0~100µM
Incubation time 2h
Animal Experiment
Animal models PLC/PRF/5, hepatocellular carcoma (HCC) xenograft model with NCI SCID female mice
Formulation saline (0.9% NaCl)
Dosages 50 mg/kg, QD 5/wk*2 wks
Administration intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 449.04
Formula C9H16Br2N5O4P
CAS Number 918633-87-1
Purity 100.00%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C

Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer.
Sun JD, et al. Clin Cancer Res. 2012 Feb 1;18(3):758-70. PMID: 22184053.

Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302.
Meng F, et al. Mol Cancer Ther. 2012 Mar;11(3):740-51. PMID: 22147748.

Targeting the multiple myeloma hypoxic niche with TH-302, a hypoxia-activated prodrug.
Hu J, et al. Blood. 2010 Sep 2;116(9):1524-7. PMID: 20530289.

Related Products

17 alpha-Estradiol is a 5α-reductase inhibitor, and it inhibits testosterone metabolism catalyzed by 5 alpha-reductase.

Rebaudioside M

Rebaudioside M is a natural non-calorie sweetener isolated from Stevia rebaudiana Bertoni, it is a glycoside of the ent-kaurene diterpenoid aglycone.

β-Aminopropionitrile (Liquid)

β-Aminopropionitrile is a specific and irreversible lysyl oxidase (LOX) inhibitor.


1-Phenyl-2-thiourea is a useful biochemical for proteomics research.


Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.

Abmole Inhibitor Catalog 2017

Keywords: TH-302 (Evofosfamide), Evofosfamide supplier, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.