Tivozanib hydrate  (Synonyms: AV-951 hydrate; KRN951 hydrate)

Tivozanib hydrate (AV-951 hydrate; KRN951 hydrate) is the hydrate form of Tivozanib (HY-10977). Tivozanib hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC₅₀s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrate exhibits antitumor efficacy^[1].

Tivozanib hydrate 抑制 VEGFR-1、VEGFR-2 和 VEGFR-3 的磷酸化，IC₅₀ 为 0.16-0.24 nM^[1]。
Tivozanib hydrate (0-100 nM，24 h) 抑制 VEGF 诱导的 HUVEC 增殖，IC₅₀ 为 0.67 nM，并以剂量依赖性的方式抑制 HUVEC 迁移^[1]。
Tivozanib hydrate (0-300 nM, 1 h) 配体依赖性地选择性抑制内皮细胞中 VEGF 刺激的 MAPK 磷酸化，抑制 ERK1 和 ERK2 活性，IC₅₀ 为 0.13 和 0.18 nM^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tivozanib hydrate (0.04-1 mg/kg，口服 14 天) 在无胸腺小鼠模型对乳腺癌、结肠癌、肝癌、肺癌、卵巢癌、胰腺癌和前列腺癌具有抗癌活性^[1]。
Tivozanib hydrate (0.2-1 mg/kg，口服 21 天) 可逆性抑制 Calu-6 荷瘤大鼠模型中的血管通透性和血管生成^[1]。
Tivozanib hydrate (5 mg/kg，口服，单剂量) 在无胸腺小鼠模型中的药代动力学特征为 AUC_inf 为 44.5 μg·h/mL，C_max 为 2823 ng/mL^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

472.88

C₂₂H₂₁ClN₄O₆

682745-40-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nakamura K, et al., KRN951, a highly potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, has antitumor activities and affects functional vascular properties. Cancer Res. 2006 Sep 15;66(18):9134-42.  [Content Brief]