1: Saggar JK, Tannock IF. Activity of the hypoxia-activated pro-drug TH-302 in hypoxic and perivascular regions of solid tumors and its potential to enhance therapeutic effects of chemotherapy. Int J Cancer. 2014 Jun 1;134(11):2726-34. doi: 10.1002/ijc.28595. Epub 2013 Dec 13. PubMed PMID: 24338277.
2: Portwood S, Lal D, Hsu YC, Vargas R, Johnson MK, Wetzler M, Hart CP, Wang ES. Activity of the hypoxia-activated prodrug, TH-302, in preclinical human acute myeloid leukemia models. Clin Cancer Res. 2013 Dec 1;19(23):6506-19. doi: 10.1158/1078-0432.CCR-13-0674. Epub 2013 Oct 2. PubMed PMID: 24088735.
3: Hu J, Van Valckenborgh E, Xu D, Menu E, De Raeve H, De Bryune E, Xu S, Van Camp B, Handisides D, Hart CP, Vanderkerken K. Synergistic induction of apoptosis in multiple myeloma cells by bortezomib and hypoxia-activated prodrug TH-302, in vivo and in vitro. Mol Cancer Ther. 2013 Sep;12(9):1763-73. doi: 10.1158/1535-7163.MCT-13-0123. Epub 2013 Jul 5. PubMed PMID: 23832122.
4: Cárdenas-Rodríguez J, Li Y, Galons JP, Cornnell H, Gillies RJ, Pagel MD, Baker AF. Imaging biomarkers to monitor response to the hypoxia-activated prodrug TH-302 in the MiaPaCa2 flank xenograft model. Magn Reson Imaging. 2012 Sep;30(7):1002-9. doi: 10.1016/j.mri.2012.02.015. Epub 2012 May 1. PubMed PMID: 22554971; PubMed Central PMCID: PMC3402593.
5: Liu Q, Sun JD, Wang J, Ahluwalia D, Baker AF, Cranmer LD, Ferraro D, Wang Y, Duan JX, Ammons WS, Curd JG, Matteucci MD, Hart CP. TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules. Cancer Chemother Pharmacol. 2012 Jun;69(6):1487-98. doi: 10.1007/s00280-012-1852-8. Epub 2012 Mar 2. PubMed PMID: 22382881; PubMed Central PMCID: PMC3985381.
6: Jung D, Jiao H, Duan JX, Matteucci M, Wang R. Metabolism and excretion of TH-302 in dogs. Xenobiotica. 2012 Jul;42(7):687-700. doi: 10.3109/00498254.2011.650234. Epub 2012 Feb 21. PubMed PMID: 22352389.
7: Sun JD, Liu Q, Wang J, Ahluwalia D, Ferraro D, Wang Y, Duan JX, Ammons WS, Curd JG, Matteucci MD, Hart CP. Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer. Clin Cancer Res. 2012 Feb 1;18(3):758-70. doi: 10.1158/1078-0432.CCR-11-1980. Epub 2011 Dec 19. PubMed PMID: 22184053.
8: Meng F, Evans JW, Bhupathi D, Banica M, Lan L, Lorente G, Duan JX, Cai X, Mowday AM, Guise CP, Maroz A, Anderson RF, Patterson AV, Stachelek GC, Glazer PM, Matteucci MD, Hart CP. Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302. Mol Cancer Ther. 2012 Mar;11(3):740-51. doi: 10.1158/1535-7163.MCT-11-0634. Epub 2011 Dec 6. PubMed PMID: 22147748.
9: Jung D, Jiao H, Duan JX, Matteucci M, Wang R. Metabolism, pharmacokinetics and excretion of a novel hypoxia activated cytotoxic prodrug, TH-302, in rats. Xenobiotica. 2012 Apr;42(4):372-88. doi: 10.3109/00498254.2011.622810. Epub 2011 Oct 17. PubMed PMID: 22004352.
10: Jung D, Lin L, Jiao H, Cai X, Duan JX, Matteucci M. Pharmacokinetics of TH-302: a hypoxically activated prodrug of bromo-isophosphoramide mustard in mice, rats, dogs and monkeys. Cancer Chemother Pharmacol. 2012 Mar;69(3):643-54. doi: 10.1007/s00280-011-1741-6. Epub 2011 Oct 1. PubMed PMID: 21964906.

Chemical
CAS Num	918633-87-1
Chemical Formula	C9H16Br2N5O4P
Molecular Weight	449.04
IUPAC Chemical Name	Phosphorodiamidic acid, N,N'-bis(2-bromoethyl)-, (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester.
Exact Mass	446.93067
Elemental Analysis	C, 24.07; H, 3.59; Br, 35.59; N, 15.60; O, 14.25; P, 6.90
Synonym	TH302; TH 302; TH-302. Evofosfamide
Solubility	Soluble in DMSO, not in water
SMILES Code	O=P(NCCBr)(NCCBr)OCC1=CN=C([N+]([O-])=O)N1C
Biological
Targets and Effects	N/A
Pathways	alkylating agent
Physical
Appearance	Solid powder
Purity	>98% (or refer to the Certificate of Analysis)
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition	Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf Life	>2 years if stored properly