Home Cell Cycle CDK4/6 inhibitor Auceliciclib (AU3-14,Ulecaciclib )

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Auceliciclib (AU3-14,Ulecaciclib ) CDK4/6 inhibitor

Cat.No.E6639

Ulecaciclib is an orally active cyclin-dependent kinase (CDK) inhibitor with Ki values of 0.62 μM for CDK2/Cyclin A, 0.2 nM for CDK4/Cyclin D1, 3 nM for CDK6/Cyclin D3, and 0.63 μM for CDK7/Cyclin H. This compound demonstrates blood-brain barrier penetration and favorable pharmacokinetic properties.
Auceliciclib (AU3-14,Ulecaciclib ) CDK4/6 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 496.65

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Chemical Information, Storage & Stability

Molecular Weight 496.65 Formula

C25H33FN8S

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CAS No. 2075750-05-7 Download SDF Storage of Stock Solutions

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Mechanism of Action

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 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 monkeys
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