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Formula | C24H29N7O2.HCl |
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Molecular Weight | 483.99 | CAS No. | 827022-32-2 | |
Solubility (25°C)* | In vitro | Water | 24 mg/mL (49.58 mM) | |
DMSO | 5 mg/mL (10.33 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. | ||||||
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Targets |
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In vitro | PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-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 μM. 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 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. [2] 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. [3] A recent study shows that 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. [4] | ||||||
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] | ||||||
Features | Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers). |
Kinase Assay: |
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Data from [Pharmacogenomics J, 2013, 13(1), 94-104]
Data from [Clin Transl Oncol, 2012, 14(3), 197-206 ]
Data from [Clin Cancer Res, 2011, 17(13), 4513-22]
, , Dr. Gao Zhang of University of Pennsylvania
An intermediate Rb-E2F activity state safeguards proliferation commitment [ Nature, 2024, 631(8020):424-431] | PubMed: 38926571 |
Defining the KRAS- and ERK-dependent transcriptome in KRAS-mutant cancers [ Science, 2024, 384(6700):eadk0775] | PubMed: 38843331 |
Chronic stress increases metastasis via neutrophil-mediated changes to the microenvironment [ Cancer Cell, 2024, S1535-6108(24)00037-0] | PubMed: 38402610 |
Cyclin-dependent kinase 4 drives cystic kidney disease in the absence of mTORC1 signaling activity [ Kidney Int, 2024, S0085-2538(24)00627-6] | PubMed: 39218392 |
Reciprocal antagonism of PIN1-APC/CCDH1 governs mitotic protein stability and cell cycle entry [ Nat Commun, 2024, 15(1):3220] | PubMed: 38622115 |
A renal clearable fluorogenic probe for in vivo β-galactosidase activity detection during aging and senolysis [ Nat Commun, 2024, 15(1):775] | PubMed: 38278798 |
Uncoupling of mTORC1 from E2F activity maintains DNA damage and senescence [ Nat Commun, 2024, 15(1):9181] | PubMed: 39448567 |
Comprehensive multi-omics analysis reveals WEE1 as a synergistic lethal target with hyperthermia through CDK1 super-activation [ Nat Commun, 2024, 15(1):2089] | PubMed: 38453961 |
Type II topoisomerases shape multi-scale 3D chromatin folding in regions of positive supercoils [ Mol Cell, 2024, S1097-2765(24)00830-X] | PubMed: 39486417 |
A p38 MAPK-ROS axis fuels proliferation stress and DNA damage during CRISPR-Cas9 gene editing in hematopoietic stem and progenitor cells [ Cell Rep Med, 2024, 5(11):101823] | PubMed: 39536752 |
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