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PDGFR-IN-1

CAS No. : 2644673-07-2

MCE 站：PDGFR-IN-1

产品活性：PDGFR-IN-1 (compound 7m) 是一种口服有效的 PDGFR (血小板源性生长因子受体) 抑制剂, PDGFRα 和 PDGFRβ 的 IC₅₀ 分别为 2.4 和 0.9 nM。PDGFR-IN-1 具有较强的抗肿瘤作用和低毒性，可用于骨肉瘤的研究。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：PDGFR  |  Apoptosis

In Vitro: PDGFR-IN-1 (compound 7m) (0-0.4 μM, 48 h) inhibits osteosarcoma cancer cells (U2OS, MG63, MNNG/HOS, ａnd SAOS-2) proliferation ａnd colony formation.
PDGFR-IN-1 (0-0.4 μM, 48 h) induces cell-cycle arrest in a dose-dependent manner.
PDGFR-IN-1 (0-1.6 μM, 48 h) induces MNNG/HOS ａnd MG63 cell apoptosis in a dose-dependent manner.
PDGFR-IN-1 (0-0.4 μM, 15 min) inhibits the expression of α-tubulin in both MNNG/HOS ａnd MG63 cells.
PDGFR-IN-1 (0-0.4 μM, 48 h) inhibits PDGFRβ phosphorylation ａnd downstream signaling transduction (p-STAT3, p-AKT, ａnd p-ERK).
PDGFR-IN-1 (0-0.4 μM, 48 h) significantly inhibits osteosarcoma cancer cell migration ａnd invasion by downregulating the expression of FAK, as well as the distribution in the leading edge of cells.

In Vivo: PDGFR-IN-1 (BALB/c mice, MNNG/HOS xenograft mouse, 15, 30 mg/kg, orally, daily for 14 days) significantly suppresses tumor growth, exhibits a stronger antitumor efficacy with low toxicity.
PDGFR-IN-1 (C57/BL6 mice, 40, 80 mg/kg, orally, daily for 10 days) is safe for in vivo investigations.
PDGFR-IN-1 (Sprague-Dawley rats, 20 mg/kg PO or 4 mg/kg IP, once) shows a favorable profile with a high maximum concentration ａnd exposure, an acceptable half-life , ａnd a good oral bioavailability.
Pharmacokinetic Parameters of PDGFR-IN-1 in male Sprague-Dawley rats.

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