Ulecaciclib 

Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with K_i 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^[1][2][3].

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^[2].
Ulecaciclib (72 h) exhibits a strong antiproliferative activity against leukemia cells with a growth inhibition GI₅₀ value of 10 nM^[2].
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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].
Ulecaciclib (200 mg/kg; p.o.; daily; 21 d) displays in vivo anti-tumour efficacy in mice^[2].
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^[2].
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 ng•h/mL in male cynomolgus monkeys^[3].
Pharmacokinetic of Ulecaciclib in cynomolgus monkeys^[3]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

496.65

C₂₅H₃₃FN₈S

2075750-05-7

FC1=C(C2=C(C)N=C(NC3CCCC3)S2)N=C(NC4=NC=C(CN5CCN(CC5)CC)C=C4)N=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information. 2022. 36(2):337.

  [2]. Wang Shudong, et al. Treatment of proliferative diseases of the CNS using a class of thiazole-pyrimidine compounds that inhibit the activity of CDK4 and/or CDK6[P]. World Intellectual Property Organization, WO2021222967 A1 2021-11-11.

  [3]. Wang Shudong, et al. Succinate and crystal form thereof as therapeutics[P]. World Intellectual Property Organization, WO2022099357 A1 2022-05-19.