产品
编 号：F748686
分子式：C25H33FN8S
分子量：496.65
分子式：C25H33FN8S
分子量：496.65
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CAS No: 2075750-05-7
产品详情
生物活性：
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
体内研究：
Ulecaciclib (compound 2) (2 mg/kg for i.v.; 10 mg/kg for p.o.) demonstrates a significantly propensity to cross the blood brain barrier in mice, with the brain/plasma ratios are >1.2 (i.v.) or >0.7 (p.o.), respectively.Ulecaciclib (200 mg/kg; p.o.; daily; 21 d) displays in vivo anti-tumour efficacy in mice.Ulecaciclib (25 mg/kg; p.o.; daily; 10 d) demonstrates significant anti-tumour efficacy at lower doses in combination with TMZ (5 mg/kg; p.o.; 5 d/week; 2 weeks) in mice.Ulecaciclib (compound A) (50 mg/kg; p.o.) shows an oral bioavailability of about 21.8%, and good pharmacokinetic profile with Tmax of 6.67 h and an half- of 8.34 h, while Cmax =643 ng/mL, AUC(0-24) =9543 ng?h/mL in male cynomolgus monkeys.Pharmacokinetic of Ulecaciclib in cynomolgus monkeysRouteDose (mg/kg)T1/2 (h)Tmax (h)Cmax (ng/mL)AUC(0-t) (h?ng/mL)AUC(0-∞) (h?ng/mL)Vd (L/kg)CL (mL/min/kg)MRT(0-t) (h)F (%)
i.v.56.53/447418745609.7919.46.64/
p.o.508.346.6764395437305//10.421.8
Animal Model:CDl nu/nu female mice (5-6 weeks old; injected with U87 GBM cells, s.c.)
Dosage:200 mg/kg
Administration:Oral gavage; daily; 21 days
Result:Reduced tumour growth markedly without any overt toxicity.
Animal Model:GBM orthotopic mouse xenograft models
Dosage:120 mg/kg
Administration:Oral gavage; daily for 2 days
Result:Inhibited tumor growth on day 21 and increased life span ratio (ILS) of 154.8% for teated mice.ILS = (DaysT - DaysC)/DaysC, where DaysC = days survived by control group and DaysT = days survived by treatment group.
体外研究：
Ulecaciclib (compound 2) (40 min) displays inhibitory effect on CDK kinase with Ki values of 0.62 μM (CDK2/A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), 0.63 μM (CDK7/H), respectively.Ulecaciclib (72 h) exhibits a strong antiproliferative activity against leukemia cells with a growth inhibition GI50 value of 10 nM.Ulecaciclib (72 h) inhibits tumor growth with GI50s range from 0.04-5.09 μM and inhibits Ovarian A2780 with an GI50 value of 40 nM, in particularly.
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
体内研究：
Ulecaciclib (compound 2) (2 mg/kg for i.v.; 10 mg/kg for p.o.) demonstrates a significantly propensity to cross the blood brain barrier in mice, with the brain/plasma ratios are >1.2 (i.v.) or >0.7 (p.o.), respectively.Ulecaciclib (200 mg/kg; p.o.; daily; 21 d) displays in vivo anti-tumour efficacy in mice.Ulecaciclib (25 mg/kg; p.o.; daily; 10 d) demonstrates significant anti-tumour efficacy at lower doses in combination with TMZ (5 mg/kg; p.o.; 5 d/week; 2 weeks) in mice.Ulecaciclib (compound A) (50 mg/kg; p.o.) shows an oral bioavailability of about 21.8%, and good pharmacokinetic profile with Tmax of 6.67 h and an half- of 8.34 h, while Cmax =643 ng/mL, AUC(0-24) =9543 ng?h/mL in male cynomolgus monkeys.Pharmacokinetic of Ulecaciclib in cynomolgus monkeysRouteDose (mg/kg)T1/2 (h)Tmax (h)Cmax (ng/mL)AUC(0-t) (h?ng/mL)AUC(0-∞) (h?ng/mL)Vd (L/kg)CL (mL/min/kg)MRT(0-t) (h)F (%)
i.v.56.53/447418745609.7919.46.64/
p.o.508.346.6764395437305//10.421.8
Animal Model:CDl nu/nu female mice (5-6 weeks old; injected with U87 GBM cells, s.c.)
Dosage:200 mg/kg
Administration:Oral gavage; daily; 21 days
Result:Reduced tumour growth markedly without any overt toxicity.
Animal Model:GBM orthotopic mouse xenograft models
Dosage:120 mg/kg
Administration:Oral gavage; daily for 2 days
Result:Inhibited tumor growth on day 21 and increased life span ratio (ILS) of 154.8% for teated mice.ILS = (DaysT - DaysC)/DaysC, where DaysC = days survived by control group and DaysT = days survived by treatment group.
体外研究：
Ulecaciclib (compound 2) (40 min) displays inhibitory effect on CDK kinase with Ki values of 0.62 μM (CDK2/A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), 0.63 μM (CDK7/H), respectively.Ulecaciclib (72 h) exhibits a strong antiproliferative activity against leukemia cells with a growth inhibition GI50 value of 10 nM.Ulecaciclib (72 h) inhibits tumor growth with GI50s range from 0.04-5.09 μM and inhibits Ovarian A2780 with an GI50 value of 40 nM, in particularly.
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