产品
编 号：F743060
分子式：C24H30ClN6O2P
分子量：500.96
分子式：C24H30ClN6O2P
分子量：500.96
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CAS No: 1197958-53-4
产品详情
生物活性：
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
体内研究：
ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity.ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC0-∞, CL, t1/2 and Vss are 3039 ng?h/mL, 0.91 h?kg, 6.6 hours and 6.12 L/kg, respectively.ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows Cmax, AUC0-∞, tmax, t1/2 and F are 3254 ng/mL, 4056 ng?h/mL, 6.0 hours, 12.5 hours and 39%, respectively.Animal Model:Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)
Dosage:10-50 mg/kg
Administration:Orally; once daily for 13 consecutive days
Result:Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).
体外研究：
ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC50 of 28.3 nM.
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
体内研究：
ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity.ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC0-∞, CL, t1/2 and Vss are 3039 ng?h/mL, 0.91 h?kg, 6.6 hours and 6.12 L/kg, respectively.ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows Cmax, AUC0-∞, tmax, t1/2 and F are 3254 ng/mL, 4056 ng?h/mL, 6.0 hours, 12.5 hours and 39%, respectively.Animal Model:Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)
Dosage:10-50 mg/kg
Administration:Orally; once daily for 13 consecutive days
Result:Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).
体外研究：
ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC50 of 28.3 nM.
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