Palbociclib-d4

Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].

Product Specifications

CAS Number

[1628752-63-5]

Product Name Alternative

PD 0332991-d4

UNSPSC

12352005

Target

CDK; Isotope-Labeled Compounds

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Others

Field of Research

Cancer

Smiles

O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CC([2H])(NC([2H])(C5)[2H])[2H])C

Molecular Formula

C24H25D4N7O2

Molecular Weight

451.56

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3 (11) :1427-38. |[3]Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548 (7668) :471-475. |[4]Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11 (5) :R77. |[5]Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66 (7) :1286-1296.