TH-302 | CAS:918633-87-1

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Name:TH-302; Evofosfamide
Cat. No. :CS-0616
CAS No. :918633-87-1
Formula:C9H16Br2N5O4P
M. Wt. : 449.04
Solubility:DMSO; H2O: 0.14 mg/mL

TH-302 is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.IC50 & Target: Hypoxia-activated prodrug[1]In Vitro: TH-302 induces γH2AX and apoptosis. TH-302 displays hypoxia-selective and concentration-dependent cytotoxic activity that is comparable in both p53-proficient and -deficient cells. Treatment with TH-302 alone causes an accumulation of G2/M cells. Inhibition of Chk1 by PF47736 in cells treated with TH-302 reduces TH-302-mediated G2/M arrest under both normoxia and hypoxia[1].In Vivo: TH-302 is a hypoxia-activated prodrug known to activate selectively under the hypoxic conditions commonly found in solid tumors. The mean values of normalized Ktrans decrease 69.2% for TH-302-treated mice in Hs766t tumors, decrease 46.1% for Mia PaCa-2 tumors and increase 4.9% in SU.86.86 tumors. Both changes for Hs766t and Mia PaCa-2 treatment groups are statistically significant (P[2]. A significant reduction in the hypoxic fraction (HF) to 2.1%±4.7% is seen after 95% oxygen breathing (P2)[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. 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. Meng F, et al. Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition. BMC Cancer. 2015 May 21;15:422.