TH-302 free base · Synonyms: Evofosfamide

Evofosfamide (TH-302) is a hypoxia-activated proagent with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.

For research use only. Not for human or veterinary use.

Target Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

TH-302 structure

CAS No.: 918633-87-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 450.00	BP-02102-250mg	In stock	Get quote
500 mg	USD 850.00	BP-02102-500mg	In stock	Get quote
1 g	USD 1,180.00	BP-02102-1g	In stock	Get quote
2 g	USD 1,980.00	BP-02102-2g	In stock	Get quote
5 g	Inquire	BP-02102-5g	In stock	Inquire

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Description

Evofosfamide (TH-302) is a hypoxia-activated proagent with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.

Biological activity

TH-302 is a 2-nitroimidazole triggered hypoxia-activated precursor 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.

Identifiers

SMILES: CN1C(COP(=O)(NCCBr)NCCBr)=CN=C1[N+]([O-])=O
InChIKey: UGJWRPJDTDGERK-UHFFFAOYSA-N

Specifications

MW (average): 449.0360
Formula: C₉H₁₆Br₂N₅O₄P
CAS No.: 918633-87-1
Physical state: Solid
Color: White to yellow
Shipping: 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: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO/water

In vitro: DMSO : 94 mg/mL H2O : 4.35 mg/mL

Documents

References

[1]. Meng F, et al. Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition. BMC Cancer. 2015 May 21;15:422.

[2]. Zhang X, et al. MR Imaging Biomarkers to Monitor Early Response to Hypoxia-Activated Prodrug TH-302 in Pancreatic Cancer Xenografts. PLoS One. 2016 May 26;11(5):e0155289.

[3]. Peeters SG, et al. TH-302 in Combination with Radiotherapy Enhances the Therapeutic Outcome and Is Associated with Pretreatment [18F]HX4 Hypoxia PET Imaging. Clin Cancer Res. 2015 Jul 1;21(13):2984-92.

Same target

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Same research area

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