Tivozanib hydrate_product_DataBase

Bioactivity	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].
Invitro	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. 0 --> Tivozanib hydrate 相关抗体: Cell Proliferation Assay[1] Cell Line:
In Vivo	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 AUCinf 为 44.5 μg·h/mL，Cmax 为 2823 ng/mL[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	682745-40-0
Formula	C22H21ClN4O6
Molar Mass	472.88
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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Tivozanib hydrate

CAS: 682745-40-0 F: C22H21ClN4O6 W: 472.88