Pegdinetanib (BMS-844203; CT-322) 是一种选择性VEGFR-2(VEGFR) 抑制剂，对人和鼠 VEGFR-2 的Kd分别为 11 nM 和 250 nM，IC50分别为 16 nM 和 240 nM。Pegdinetanib 不与 VEGFR-1 或 VEGFR-3 结合。Pegdinetanib 具有抗肿瘤活性。
| 生物活性 | Pegdinetanib (BMS-844203; CT-322) is a selectiveVEGFR-2(VEGFR) inhibitor withKds of 11 nM and 250 nM andIC50s of 16 nM and 240 nM for human and murine VEGFR-2, respectively. Pegdinetanib does not bind toVEGFR-1orVEGFR-3. Pegdinetanib has antitumor activity[1]. |
| IC50& Target[1] | VEGFR2 11 nM (Kd) | VEGFR2 14 nM (IC50) | mVEGFR-2 250 nM (Kd) | mVEGFR-2 240 nM (IC50) |
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体外研究
(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. |
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体内研究
(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. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
