Toceranib Phosphate

产品编号 T7394Cas号 874819-74-6

别名 SU11654 phosphate, PHA 291639 phosphate, 托西尼布磷酸盐

Toceranib Phosphate (SU11654 phosphate) 是有效的、具有口服活性的酪氨酸激酶 (RTK) 受体抑制剂，能抑制PDGFR，VEGFR，Kit，抑制 PDGFRβ 和 Flk-1/KDR 的Ki 分别为 5 nM 和 6 nM。它具有抗肿瘤和抗血管生成作用，可用于研究犬肥大细胞肿瘤。

Toceranib Phosphate

产品编号 T7394别名 SU11654 phosphate, PHA 291639 phosphate, 托西尼布磷酸盐Cas号 874819-74-6

规格	价格	库存
5 mg	¥ 255	现货
10 mg	¥ 417	现货
25 mg	¥ 652	现货
50 mg	¥ 840	现货
100 mg	¥ 1,263	现货

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产品介绍

生物活性

产品描述	Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR
靶点活性	PDGFRβ:5 nM (Ki), FLK1:6 nM (Ki)
体内活性	在之前为正常血压的治疗犬开始使用toceranib phosphate治疗后，其收缩压显著（P = 0.0013）上升至152 mmHg ± 19，相较于基线水平136 mmHg ± 14有所增加。有37%的接受治疗的犬只发展为收缩压≥ 160 mmHg。治疗犬在开始治疗时，系统性高血压（37%）和蛋白尿（21%）的发生率与年龄相匹配的健康对照组（分别为15% [P = 0.13] 和0% [P = 0.069]）无显著差异。
动物实验	Dogs scheduled to received toceranib phosphate treatment were divided into 2 groups based on SBP recorded at screening: dogs that were normotensive were assigned to Group 2a and dogs diagnosed with HT were assigned to Group 2b. After baseline evaluation, dogs enrolled in Group 2a received toceranib phosphate at a standard dose as previously published.2 Group 2b dogs received toceranib phosphate as described, but were also treated with standard‐of‐care treatment for HT, including amlodipine besylate (0.2–0.4 mg/kg PO q 24 hours), enalapril maleate (0.5 mg/kg PO q 12 hours), or both, initiated at the discretion of the attending veterinarian. Some dogs were treated with additional medications, including corticosteroids, at the discretion of the oncologist. All dogs were re‐evaluated on Day 14 (±3 days) at which time a UPC and blood pressure measurements were performed[1].
别名	SU11654 phosphate, PHA 291639 phosphate, 托西尼布磷酸盐