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Ulecaciclib

CAS No. : 2075750-05-7

MCE 站：Ulecaciclib

产品活性：Ulecaciclib 是一种具有口服活性的细胞周期蛋白依赖激酶 (CDK) 抑制剂，对 CDKs 的 k _i 为 0.62 μM (CDK2/Cyclin A)、0.2 nM (CDK4/Cyclin D1)、3 nM (CDK6/Cyclin D3) 和 0.63 μM (CDK7/Cyclin H)。Ulecaciclib 能够通过血脑屏障，具有良好的药代动力学特性。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: Ulecaciclib (compound 2) (40 min) displays inhibitory effect on CDK kinase with K_i 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.

In Vivo: 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 T_max of 6.67 h ａnd an half- of 8.34 h, while C_max =643 ng/mL, AUC_(0-24) =9543 ngh/mL in male cynomolgus monkeys.
Pharmacokinetic of Ulecaciclib in cynomolgus monkeys

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