Palbociclib (isethionate)

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 100mg
ArtNr HY-A0065-100mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
PD0332991 isethionate, PD-0332991 isethionate, PD 0332991 isethionate
CAS No.
827022-33-3
Purity
>98%
MW
5736644
Formula
C26H35N7O6S
Solubility
10 mM in H2O
Biological Description
Palbociclib isethionate(PD-0332991 isethionate) is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases.
IC50 value: 11 nM/16 nM (Cdk4/Cdk6) [1]
Target: Cdk4/Cdk6
in vitro: ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 uM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells [1]. PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells [2]. PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16 [3].
in vivo: PD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F [1].
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Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 100mg
Lieferbar: In stock
Listenpreis: 202,14 €
Rabatt: -10,0%
Preis: 181,93 €
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