Molecular Formula | C26H35N7O6S |
Molar Mass | 573.6644 |
Appearance | powder |
Color | white to beige |
Storage Condition | room temp |
MDL | MFCD22666589 |
Use | Palbociclib (PD0332991) Isethionate is a highly selective CDK4/6 inhibitor with IC50 of 11 nM/16 nM. It has no inhibitory activity on CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
In vitro study | The PD 0332991 had absolute selectivity for CDK4/6 and little inhibitory activity against other CDKs. PD 0332991 acts on MDA-MB-435 breast cancer cells and effectively reduces Rb phosphorylation at Ser780 and Ser795 sites, with IC50 of 66 nM and 63 nM, respectively. PD 0332991 effectively inhibits cell growth and DNA replication by inhibiting cells from entering S phase. PD 0332991 inhibits thymidine penetration into DNA of Rb-positive human breast cancer (e. G., MDA-MB-435, MCF-7), colon cancer (H1299), and lung cancer (Colo-205) and leukemia (CRRF-CEM and K562), the IC50 value is 0.04-0.17 μm. PD 0332991 significantly enhanced the percentage of MDA-MB-453 in G1. PD 0332991 acts on CD138PD 0332991 to preferentially inhibit Luminal estrogen receptor positive (including HER2 positive) human breast cancer cell lines. PD 0332991 acts on most sensitive cell lines, promoting pRb and cyclin D1 gene expression, and reducing CDKN2A(p16) gene expression. PD 0332991 acts on cell lines that are conditionally resistant to ER inhibition, enhancing sensitivity to Tamoxifen. |
In vivo study | PD 0332991(150 mg/kg) acts on Colo-205 colon cancer xenografts, inducing rapid tumor regression and corresponding delay in tumor growth. PD 0332991(150 mg/kg) acts on MDA-MB-435 breast cancer, inducing total tumor arrest and cell killing. Treatment with PD 0332991(150 mg/kg) in mice bearing SF-295 glioblastoma, and ZR-75-1 breast cancer and PC-3 prostate tumor models (complete inhibition of tumor growth) significantly induced tumor regression. Treatment of MDA-MB-435 breast cancer with PD 0332991 (150 mg/kg) for more than 24 hours, inhibition of Rb in SerPD 0332991 also rapidly inhibited myeloma growth. |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
Reference Show more | 1. [IF=4.162] Suhua Wang et al."Design, Synthesis, and Biological Evaluation of 2-Anilino-4-Triazolpyrimidine Derivatives as CDK4/HDACs Inhibitors."Drug Des Dev Ther. 2022 Apr;16:1083-1097 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.743 ml | 8.716 ml | 17.432 ml |
5 mM | 0.349 ml | 1.743 ml | 3.486 ml |
10 mM | 0.174 ml | 0.872 ml | 1.743 ml |
5 mM | 0.035 ml | 0.174 ml | 0.349 ml |
biological activity | Palbociclib (PD0332991), the IC50 in the cell-free assay was 11 nM/16 nM, and there was no inhibitory activity on CDK1/2/5,EGFR,FGFR,PDGFR, InsR, etc. Phase 3. |
Target | Value |
CDK4/CyclinD3 (Cell-free assay) | 9 nM |
CDK4/CyclinD1 (Cell-free assay) | 11 nM |
CDK6/CyclinD2 (Cell-free assay) | 15 nM |