Toceranib 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, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR

Systolic blood pressure was significantly (P = 0.0013) higher in previously normotensive treatment dogs after initiation of treatment with toceranib phosphate (152 mmHg ± 19) compared to baseline (136 mmHg ± 14). 37% of treated dogs developed SBP ≥ 160 mmHg. The prevalence of systemic hypertension (37%) and proteinuria (21%) at baseline in treatment dogs did not differ from that of age-matched healthy controls (15% [P = 0.13] and 0% [P = 0.069], respectively)[1].

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].

874819-74-6

C22H28FN4O6P

494.46

SU11654 phosphate;PHA 291639 phosphate;托西尼布磷酸盐

DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years