Pegdinetanib
Names
[ CAS No. ]:
906450-24-6
[ Name ]:
Pegdinetanib
Biological Activity
[Description]:
Pegdinetanib (BMS-844203; CT-322) is a selective VEGFR-2 (VEGFR) inhibitor with Kds of 11 nM and 250 nM and IC50s of 16 nM and 240 nM for human and murine VEGFR-2, respectively. Pegdinetanib does not bind to VEGFR-1 or VEGFR-3. Pegdinetanib has antitumor activity[1].
[Related Catalog]:
[Target]
VEGFR2:11 nM (Kd)
VEGFR2:14 nM (IC50)
mVEGFR-2:250 nM (Kd)
mVEGFR-2:240 nM (IC50)
[In Vitro]
Pegdinetanib（CT-322；55 nM；72 小时）抑制 VEGF-A 诱导的 HUVEC 增殖[1]。 Pegdinetanib (CT-322; 0.36-24 nM) 阻断人脐带血管内皮细胞中 VEGF 诱导的 VEGFR-2 磷酸化和丝裂原活化蛋白激酶[1]。 Western Blot Analysis[1] Cell Line: Human umbilical vein endothelial cells (HUVEC) Concentration: 0.36 nM, 1.5 nM, 6 nM, 12 nM, 24 nM Incubation Time: Pre-incubated for 30 min Result: Blocked the level of phosphorylated VEGFR-2.
[In Vivo]
Pegdinetanib（CT-322；3-30 mg/kg；腹腔注射；每隔一天；持续 20 天）显着抑制裸鼠中已建立的 U87 人胶质母细胞瘤异种移植物的生长[1]。 Animal Model: Female athymic NCRNU-M-F nude mice (Six to eight-week-old) injected with U87 glioblastoma[1] Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: i.p.; every other day; for 20 days Result: Significantly inhibits growth of established U87 human glioblastoma xenografts in nude mice.
[References]
Chemical & Physical Properties
No Any Chemical & Physical Properties
Related Compounds
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