Auceliciclib (AU3-14,Ulecaciclib )

Catalog No.E6639

Technical Data

Formula	C25H33FN8S
Molecular Weight	496.65	CAS No.	2075750-05-7
Solubility (25°C)*	In vitro


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Biological Activity

Description	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.
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

Description

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.

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

Protocol (from reference)

References

https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl127.pdf?sfvrsn=8544ca1e_3&download=true
https://www.freepatentsonline.com/WO2021222967A1.html
https://www.freepatentsonline.com/WO2022099357A1.html

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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