Culmerciclib | CDK4/6 inhibitor | Probechem Biochemicals

Chemical Structure : Culmerciclib

Culmerciclib (TQB3616, TQB 3616)

Catalog No.: PC-49131Not For Human Use, Lab Use Only.

TQB3616 (Culmerciclib) is a potent, selective inhibitor of CDK4/6 with IC50 of 0.35 nM and 0.49 nM for CDK4/D1CDK6/D1 respectively, shows remarkable inhibitory effect on hormone receptor-positive breast cancer cells.

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Biological Activity

TQB3616 (Culmerciclib) is a potent, selective inhibitor of CDK4/6 with IC50 of 0.35 nM and 0.49 nM for CDK4/D1CDK6/D1 respectively, shows remarkable inhibitory effect on hormone receptor-positive breast cancer cells.

TQB3616 shows enzymatic inhibitory IC50 of 246 nM, 35.3 nM, and 12.5 nM against CDK1/cyclin B, CDK5/p25, and CDK9/cyclin T1 respectively,

TQB3616 potently inhibits tumor cell proliferation for T47D cells (IC50=82.4 nM) and MCF-7 cells (IC50=115.5 nM).

TQB3616 shows better inhibitory activity in the HER2-positive /HR-positive breast cancer cells than abemaciclib.

TQB3616 (1.5 uM) reduces colony formation of T47D and BT474 cells, inhibits the abnormal activation of phosphorylated Cyclin D protein.

TQB3616 not only induced G1 stalling, leading to a profound reduction in the level of RB protein phosphorylated at Ser807/811, but also showed enhanced tumor killing effects by promoting cell apoptosis.

TQB3616 showed more potent antitumor activity than abemaciclib in an in vitro breast cancer xenograft model.

Physicochemical Properties

M.Wt	446.534
Formula	C24H27FN8
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-fluoro-4-[2-methyl-3-(propan-2-yl)-2H-indazol-5-yl]-N-[5-(piperazin-1-yl)pyridin-2-yl]pyrimidin-2-amine

References

1. Patent WO2021259203 A1 2021-12-30.
2. Patent WO2016141881 A1 2016-09-15.
3. Xu Z, et al. Bioorg Med Chem Lett. 2024 Apr 24:129769.

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Culmerciclib (TQB3616, TQB 3616)

Biological Activity

Physicochemical Properties

References

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