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TH-302 (Evofosfamide)

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

Evofosfamide

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 68  USD68 In stock
5mg USD 128  USD128 In stock
10mg USD 168  USD168 In stock
50mg USD 490  USD490 In stock
100mg USD 750  USD750 In stock
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Quality Control & Documentation
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
Protocol (for reference only)
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
Chemical Information
Molecular Weight 449.04
Formula C9H16Br2N5O4P
CAS Number 918633-87-1
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Sun JD, et al. Clin Cancer Res. Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer.

[2] Meng F, et al. Mol Cancer Ther. Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302.

[3] Hu J, et al. Blood. Targeting the multiple myeloma hypoxic niche with TH-302, a hypoxia-activated prodrug.

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