Pz-1 是 VEGFR2 和 RET 酪氨酸激酶的抑制剂,可阻断 RET 刺激生长所需的血液供应。
产品描述
Pz-1 is an inhibitor of VEGFR2 and RET (rearranged during transfection) tyrosine kinase that blocks the blood supply required for RET-stimulated growth.
体外活性
Pz-1(1.0 nM) strongly inhibited phosphorylation of all tested RET oncoproteins in cell-based assays with IC50s of less than 1 nM for both VEGFR2 and RET wild type kinases[1].
体内活性
Pz-1 (1.0 mg/kg) abrogated the formation of tumors induced by RET-mutant fibroblasts and blocked the phosphorylation of both RET and VEGFR2 in tumor tissue. Pz-1 featured no detectable toxicity at concentrations of up to 100.0 mg/kg[1].
Cas No.
1800505-64-9
分子式
C26H26N6O2
分子量
454.52
储存和溶解度
DMSO:45 mg/mL (99.01 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years