TH-302

    
99%

TH-302

源叶(MedMol)
S81103 一键复制产品信息
918633-87-1
C9H16Br2N5O4P
449.04
(1-methyl-2-nitro-1H-imidazol-5-yl)methyl N,N-bis(2-bromoethyl)phosphordiamidate
货号 规格 价格 上海 北京 武汉 南京 购买数量
S81103-1mg 99% ¥300.00 5 - - -
S81103-2mg 99% ¥500.00 8 - - -
S81103-5mg 99% ¥750.00 8 - - -
S81103-10mg 99% ¥1150.00 7 - - -
S81103-25mg 99% ¥2400.00 6 - - -
S81103-50mg 99% ¥3700.00 货期:2-3天 - - -
S81103-100mg 99% ¥6500.00 货期:2-3天 - - -
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产品介绍

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

产品描述: Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
靶点: Hypoxia-activated prodrug;Apoptosis; Others
体内研究: Evofosfamide (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 Evofosfamide (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<0.01) when compare to their own control group. A significant reduction in the hypoxic fraction (HF) to 2.1%±4.7% is seen after 95% oxygen breathing (P<0.001), whereas 7% oxygen breathing significantly increase the HF to 29.5%±14.7% (P=0.029). Exposing rhabdomyosarcoma-bearing rats to increasing oxygen conditions abolish the effect of TH-302 and reduce the T4×SV from 20.4±3.5 to 15.3±2.5 days (P=0.007), whereas control animals have an increased T4×SV. Upon combination with radiotherapy, the T4×SV of TH-302-treated tumors decrease from 30.8±5.9 (Evofosfamide (TH-302)+radiotherapy) to 25.7±2.9 days (Evofosfamide (TH-302)+radiotherapy+95% O2).
参考文献: 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.
溶解性: DMSO  :  94  mg/mL  (209.34  mM;  Need  ultrasonic  and  warming)    H2O  :  4.35  mg/mL  (9.69  mM;  ultrasonic  and  warming  and  heat  to  60°C)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.227 ml 11.135 ml 22.27 ml
5 mM 0.445 ml 2.227 ml 4.454 ml
10 mM 0.223 ml 1.113 ml 2.227 ml
50 mM 0.045 ml 0.223 ml 0.445 ml
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