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编 号：F754640
分子式：C22H23FN8
分子量：418.47
分子式：C22H23FN8
分子量：418.47
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CAS No: 2688098-11-3
产品详情
生物活性：
CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).
体内研究：
CDK4/6-IN-10 (1000, 5000, 10000 mg/kg; p.o.) shows safety profile with LD50 much higher than 10,000 mg/kg.CDK4/6-IN-10 (10 mg/kg; p.o.) shows oral bioavailability (F=51%) in SD rats.CDK4/6-IN-10 (100, 200 mg/kg; p.o., once a day for 19 days) shows antitumor potency and favorable safety profile.Pharmacokinetic Parameters of CDK4/6-IN-10 in SpragueeDawley rats.CompdAdmin. Cmax (ng/mL) AUC0-t (h·ng/mL)MRT0-t (h)Tmax (h)t1/2 (h)CL (mL/h/kg)F (%)
32i.v.3559605.90.0338.9641-
p.o.2574,87812.810.7>2452451
SpragueeDawley rats, 10 mg/kg, p.o.Animal Model:ICR mice
Dosage:1000, 5000, 10000 mg/kg
Administration:p.o.
Result:Showed safety profile with LD50 much higher than 10,000 mg/kg.
Animal Model:SpragueeDawley rats
Dosage:10 mg/kg
Administration:p.o.
Result:Showed oral bioavailability (F=51%).
Animal Model:BALB/c nude mice (6-8 weeks) (MM xenograft model)
Dosage:100, 200 mg/kg
Administration:p.o., once a day, 19 days
Result:Showed antitumor potency and favorable safety profile.
体外研究：
CDK4/6-IN-10 (compouns 32) (1 μM) shows kinase selectivity with IC50s of 22 nM and 10 nM for CDK4 and CDK6, respectively.CDK4/6-IN-10 (72 h) shows antiproliferative activity (GI50s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 μM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively).CDK4/6-IN-10 (0, 1.5, 3, 6 μM, 24 h) induces cell cycle arrest at the G1 phase in a concentration-dependent manner.CDK4/6-IN-10 ( 0, 1, 2, 3 μM, 24 h) induces apoptosis of RPMI-8226 cells in a concentration-dependent manner.CDK4/6-IN-10 (0, 1.5, 3, 6 μM, 24 h) reduces the CDK4/6 activity by decreases the expression level of p-RB, c-MYC and BCL-2.
CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).
体内研究：
CDK4/6-IN-10 (1000, 5000, 10000 mg/kg; p.o.) shows safety profile with LD50 much higher than 10,000 mg/kg.CDK4/6-IN-10 (10 mg/kg; p.o.) shows oral bioavailability (F=51%) in SD rats.CDK4/6-IN-10 (100, 200 mg/kg; p.o., once a day for 19 days) shows antitumor potency and favorable safety profile.Pharmacokinetic Parameters of CDK4/6-IN-10 in SpragueeDawley rats.CompdAdmin. Cmax (ng/mL) AUC0-t (h·ng/mL)MRT0-t (h)Tmax (h)t1/2 (h)CL (mL/h/kg)F (%)
32i.v.3559605.90.0338.9641-
p.o.2574,87812.810.7>2452451
SpragueeDawley rats, 10 mg/kg, p.o.Animal Model:ICR mice
Dosage:1000, 5000, 10000 mg/kg
Administration:p.o.
Result:Showed safety profile with LD50 much higher than 10,000 mg/kg.
Animal Model:SpragueeDawley rats
Dosage:10 mg/kg
Administration:p.o.
Result:Showed oral bioavailability (F=51%).
Animal Model:BALB/c nude mice (6-8 weeks) (MM xenograft model)
Dosage:100, 200 mg/kg
Administration:p.o., once a day, 19 days
Result:Showed antitumor potency and favorable safety profile.
体外研究：
CDK4/6-IN-10 (compouns 32) (1 μM) shows kinase selectivity with IC50s of 22 nM and 10 nM for CDK4 and CDK6, respectively.CDK4/6-IN-10 (72 h) shows antiproliferative activity (GI50s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 μM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively).CDK4/6-IN-10 (0, 1.5, 3, 6 μM, 24 h) induces cell cycle arrest at the G1 phase in a concentration-dependent manner.CDK4/6-IN-10 ( 0, 1, 2, 3 μM, 24 h) induces apoptosis of RPMI-8226 cells in a concentration-dependent manner.CDK4/6-IN-10 (0, 1.5, 3, 6 μM, 24 h) reduces the CDK4/6 activity by decreases the expression level of p-RB, c-MYC and BCL-2.
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