Toceranib 是口服具有活力的受体酪氨酸激酶 (RTK) 抑制剂,能有效抑制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,用于研究犬肥大细胞肿瘤。
产品描述
Toceranib phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively), has antitumor and antiangiogenic activity.
体内活性
Administration of toceranib significantly decreased the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving toceranib and CYC demonstrated a significant increase in serum concentrations of IFN-γ, which was inversely correlated with Treg numbers after 6 weeks of combination treatment[1].
Cas No.
356068-94-5
分子式
C22H25FN4O2
分子量
396.46
别名
托西尼布;SU11654;PHA 291639E
储存和溶解度
DMSO:2.4 mg/mL (6.05 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years