PD 0332991 (Palbociclib) (Synonyms: PD0332991;PD-0332991;PD 0332991) |
Catalog No.GC15173 |
PD 0332991(Palbociclib)(PD 0332991)은 각각 IC50 값이 11 및 16nM인 경구 활성 선택적 CDK4 및 CDK6 억제제입니다. PD 0332991(Palbociclib)은 강력한 항증식 활성을 가지며 암세포에서 세포 주기 정지를 유도하여 HR 양성 및 HER2 음성 유방암 및 간세포 암종 연구에 사용할 수 있습니다.
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Cas No.: 571190-30-2
Sample solution is provided at 25 µL, 10mM.
PD-0332991 is selective and oral inhibitor of cyclin-dependent kinase 4/6 with IC50 values of 11nM and 16nM, respectively for CDK4 and CDK6 [1].
PD-0332991 is a highly specific inhibitor of CDK4/6. It is a potent anti-proliferative agent against Rb-positive tumor cells in vitro, subsequently inducing an exclusive G1 arrest. It has been reported to prevent tumor growth in disseminated human myeloma xenografts and induce G1 arrest in primary bone marrow cells [2].
PD-0332991 is also studied in breast cancer. It causes growth inhibition of ER-positive cell lines and 10/16 HER2-amplified cell lines. 100nM PD-0332991 can inhibit the phosphorylation of Rb in three more sensitive cell lines, resulting in prevention of cell cycle progression [2].
References:
[1] Ivan Diaz-Padilla, Lillian L. Siu and Ignacio Duran. Cyclin-dependent kinase inhibitors as potential targeted anticancer agents. Invest New Drugs. 2009, 27: 586–594.
[2] Richard S Finn, Judy Dering, Dylan Conklin, Ondrej Kalous, David J Cohen, Amrita J Desai, Charles Ginther, Mohammad Atefi, Isan Chen, Camilla Fowst, Gerret Los and Dennis J Slamon. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer ce
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