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编 号：F754302
分子式：C25H30N8O
分子量：458.56
分子式：C25H30N8O
分子量：458.56
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CAS No: 2644673-07-2
产品详情
生物活性：
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma.
体内研究：
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.7m
routeIPPO
dose (mg/kg)420
Cmax (ng/mL)78.375.2
t1/2 (h)2.862.12
AUC0-∞ (ng/mL*h)211.3664.7
F (%)62.9
Animal Model:Sprague-Dawley rats (male, 200-260 g, Six rats, two groups)
Dosage:20 mg/kg (PO) or 4 mg/kg (IP)
Administration:PO, IP, once (Pharmacokinetic Analysis)
Result:Showed a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability.
Animal Model:BALB/c mice (18-20 g, MNNG/HOS xenograft mouse, eight groups)
Dosage:15, 30 mg/kg
Administration:Orally, daily for 14 days
Result:Significantly suppressed tumor growth, exhibited a stronger antitumor efficacy, did not cause significant body weight or organ weight (heart, lung, liver, spleen, or kidney) changes, strongly suppressed the proliferation of tumor cells and induced apoptosis in tissues of the tumor.
Animal Model:C57/BL6 mice
Dosage:40, 80 mg/kg
Administration:Orally, daily for 10 days
Result:Did not reveal any obvious morphological aberration in organ tissues.
体外研究：
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.
PDGFR-IN-1 (compound 7m) is a potent and orally active PDGFR (platelet-derived growth factor receptor) inhibitor, with IC50 values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, respectively. PDGFR-IN-1 displays robust antitumor effects and low toxicity, and can be used to study osteosarcoma.
体内研究：
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.7m
routeIPPO
dose (mg/kg)420
Cmax (ng/mL)78.375.2
t1/2 (h)2.862.12
AUC0-∞ (ng/mL*h)211.3664.7
F (%)62.9
Animal Model:Sprague-Dawley rats (male, 200-260 g, Six rats, two groups)
Dosage:20 mg/kg (PO) or 4 mg/kg (IP)
Administration:PO, IP, once (Pharmacokinetic Analysis)
Result:Showed a favorable profile with a high maximum concentration and exposure, an acceptable half-life , and a good oral bioavailability.
Animal Model:BALB/c mice (18-20 g, MNNG/HOS xenograft mouse, eight groups)
Dosage:15, 30 mg/kg
Administration:Orally, daily for 14 days
Result:Significantly suppressed tumor growth, exhibited a stronger antitumor efficacy, did not cause significant body weight or organ weight (heart, lung, liver, spleen, or kidney) changes, strongly suppressed the proliferation of tumor cells and induced apoptosis in tissues of the tumor.
Animal Model:C57/BL6 mice
Dosage:40, 80 mg/kg
Administration:Orally, daily for 10 days
Result:Did not reveal any obvious morphological aberration in organ tissues.
体外研究：
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.
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