LCI133 | CDK4/6/9, AURKA/B inhibitor | Probechem Biochemicals

Chemical Structure : LCI133

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LCI133 (LCI-133)

货号: PC-25672Not For Human Use, Lab Use Only.

LCI133 is a highly potent, selective multikinase CDK4/6/9 and AURKA/B inhibitor with IC50 of 4.7/10.2/4.1 nM for CDK4/6/9 and 2.8/10.6 nM for AURKA/B.

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生物&药学活性

LCI133 is a highly potent, selective multikinase CDK4/6/9 and AURKA/B inhibitor with IC50 of 4.7/10.2/4.1 nM for CDK4/6/9 and 2.8/10.6 nM for AURKA/B.
LCI133 shows minimal inhibition of PI3Kδ with IC50 of 897 nM, has littile to no activity against CDK2/cyclin E, CDK7/cyclin H and DNA-PK.
LCI133 is cytotoxic to multiple cancer cell lines, arrests the cell cycle, and induces apoptosis.
LCI133 has IC50 of 0.17, 0.21, 0.19, 0.34, and 0.55 μM, in human MYCN-amplified and nonamplified NB cell lines (BE(2)-C, NGP, Kelly, SK-N-AS, and SHEP, respectively), also exhibits submicromolar activity in MCL (Jeko-1 and Mino), prostate cancer (22Rv1), and endometrial cancer (AN3 CA) cellular models.
LCI133 blocks CDK9 signaling axis and suppresses MYCN and MCL-1 transcription in MYCN-amplified neuroblastoma (NB).
LCI133 (40 mg/kg/day, i.p.) significantly reduces the growth of BE(2)-C xenografted tumors without notable change in behavior or mouse body weight.

物理化学性质&存储条件

分子量	578.67
分子式	C33H34N6O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	7-Cyclopentyl-N,N-dimethyl-2-((4-(2-morpholino-4-oxo-4H-chromen-7-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide

参考文献

1. Maddeboina K, et al. J Med Chem. 2025 Nov 6. doi: 10.1021/acs.jmedchem.5c01688.

LCI133 (LCI-133)

生物&药学活性

物理化学性质&存储条件

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LCI133 (LCI-133)

生物&药学活性

物理化学性质&存储条件

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