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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 | 50 mg/mL (103.3 mM) | |
DMSO | 13 mg/mL (26.86 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 |
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 |
Proteomic analysis reveals a PLK1-dependent G2/M degradation program and a role for AKAP2 in coordinating the mitotic cytoskeleton [ Cell Rep, 2024, 43(8):114510] | PubMed: 39018246 |
ERK hyperactivation serves as a unified mechanism of escape in intrinsic and acquired CDK4/6 inhibitor resistance in acral lentiginous melanoma [ Oncogene, 2024, 43(6):395-405] | PubMed: 38066089 |
Intracellular calcium links milk stasis to lysosome-dependent cell death during early mammary gland involution [ Cell Mol Life Sci, 2024, 81(1):29] | PubMed: 38212474 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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