VX-984 B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VX-984 是一种口服有效、选择性的、可透过血脑屏障的 DNA-PK 抑制剂。VX-984 有效抑制 NHEJ (非同源性末端接合)，增加DSBs (DNA 双链断裂)。VX-984 可用于胶质母细胞瘤 (GBM) 和非小细胞肺癌 (NSCLC) 的研究。VX-984 是一种从头设计的氘代物。

VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium.

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VX-984 (0-100 mg/kg, Oral gavage, daily) inhibits radiation-induced DNA-PKcs phosphorylation in orthotopic brain tumor xenografts.VX-984 (0-50 mg/kg, Oral gavage, twice a day for 2 days) enhances the radiosensitivity of brain tumor xenografts.Animal Model:Athymic female nude mice (6-8 weeks old, 7-8 mice/group, U251 intracerebral xenografts)Dosage:0, 50, and 100 mg/kg Administration:Oral gavage, daily, 1 or 4 hours before irradiation (10 Gy)Result:Reduced the levels DNA-PKcs phosphorylation after irradiation.Animal Model:Athymic female nude mice (6-8 weeks old, 7 mice/group, U251 intracerebral xenografts)Dosage:0, 50 mg/kg Administration:Oral gavage, twice a day, 30 minutes before and 4 hours following local irradiation of the tumor (3 Gy) for 3 consecutive days (3×3 Gy) Result:VX-984 treatment of U251 tumors alone had no significant effect on overall survival as compared with vehicle; radiation alone resulted in an increase in survival. VX-984 and radiation combination protocol increased tumor radiosensitivity, and significantly increased the survival of mice compared with radiation alone.

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Cell Cycle/DNA Damage

DNA-PK

DNA-PK

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1476074-39-1

415.49

C23H21D2N7O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 10 mg/mL (24.07 mM; 超声助溶 )

[2H]c1nc(C)nc([2H])c1-c1cc(NC[C@@H](C)c2cccc3c(ccnc23)C(=O)NC)ncn1

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(-20℃)

With Ice Pack

≥ 2 years