产品
编 号：F753021
分子式：C24H24ClN7O2
分子量：477.95
分子式：C24H24ClN7O2
分子量：477.95
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CAS No: 2468219-09-0
产品详情
生物活性：
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALKL1196M and ALKG1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research.
体内研究：
ALK-IN-22 (compound I-24) (25-50 mg/kg; i.g.; Twice daily, for 14 days) has antitumor efficacy in vivo.ALK-IN-22 (compound I-24) (10 mg/kg; p.o.) shows the Cmax and t1/2 values of 345.7 ng/mL and 4.1 hours, respectively.ALK-IN-22 (compound I-24) (2 mg/kg; i.v.) shows the CL and t1/2 values of 36.2 mL/min/kg and 2.5 hours, respectively.Animal Model:Female BALB / c nude mice
Dosage:25 and 50 mg/kg
Administration:Intragastric; Twice daily, for 14 days.
Result:The tumor growth inhibition (TGI) value of 50 mg/kg reached 93.5%.
Animal Model:SD rats
Dosage:2 and 10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration and intravenous injection
Result:1.19ParameterF16VP-16
Dose (i.v.) mg/kg1010
Cmax (ng/mL)2695217712
Tmax (min)55
AUCplasma (min*ng/mL)2878363409528
T1/2 (min)15145
Vd (L/Kg)0.23410.432
CL (L/min/kg)0.0010.007
体外研究：
ALK-IN-22 (compound I-24) (72 hours) has anti-proliferative activities against ALK-positive karpas299, H2228 and H3122 cell lines with IC50 values of 11, 37 and 27 nM, respectively.ALK-IN-22 (compound I-24) (0-100 nM; 24 hours; H2228 cells) has inhibitory effect on ALK and downstream signaling AKT and ERK.ALK-IN-22 (compound I-24) (0-100 nM; 48 hours; H2228 cells) can induce apoptosis and achieve cell cycle arrest in G1 phase.
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALKL1196M and ALKG1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research.
体内研究：
ALK-IN-22 (compound I-24) (25-50 mg/kg; i.g.; Twice daily, for 14 days) has antitumor efficacy in vivo.ALK-IN-22 (compound I-24) (10 mg/kg; p.o.) shows the Cmax and t1/2 values of 345.7 ng/mL and 4.1 hours, respectively.ALK-IN-22 (compound I-24) (2 mg/kg; i.v.) shows the CL and t1/2 values of 36.2 mL/min/kg and 2.5 hours, respectively.Animal Model:Female BALB / c nude mice
Dosage:25 and 50 mg/kg
Administration:Intragastric; Twice daily, for 14 days.
Result:The tumor growth inhibition (TGI) value of 50 mg/kg reached 93.5%.
Animal Model:SD rats
Dosage:2 and 10 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration and intravenous injection
Result:1.19ParameterF16VP-16
Dose (i.v.) mg/kg1010
Cmax (ng/mL)2695217712
Tmax (min)55
AUCplasma (min*ng/mL)2878363409528
T1/2 (min)15145
Vd (L/Kg)0.23410.432
CL (L/min/kg)0.0010.007
体外研究：
ALK-IN-22 (compound I-24) (72 hours) has anti-proliferative activities against ALK-positive karpas299, H2228 and H3122 cell lines with IC50 values of 11, 37 and 27 nM, respectively.ALK-IN-22 (compound I-24) (0-100 nM; 24 hours; H2228 cells) has inhibitory effect on ALK and downstream signaling AKT and ERK.ALK-IN-22 (compound I-24) (0-100 nM; 48 hours; H2228 cells) can induce apoptosis and achieve cell cycle arrest in G1 phase.
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