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571190-30-2,MFCD11840850
Catalog No.:AA00364P

571190-30-2 | Pd-0332991

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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00364P
Chemical Name:
Pd-0332991
CAS Number:
571190-30-2
Molecular Formula:
C24H29N7O2
Molecular Weight:
447.5328
MDL Number:
MFCD11840850
SMILES:
CC(=O)c1c(C)c2cnc(nc2n(c1=O)C1CCCC1)Nc1ccc(cn1)N1CCNCC1
Properties
Properties
 
BP:
711.5°C at 760 mmHg  
Form:
Solid  
MP:
200 ºC  
Storage:
Keep in dry area;Room Temperature;  

Computed Properties
 
Complexity:
775  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
33  
Hydrogen Bond Acceptor Count:
8  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
5  
XLogP3:
1.8  

Literature

Title: Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes.

Journal: Toxicology letters 20180701

Title: Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6.

Journal: Blood 20160609

Title: Dual Targeting of CDK4 and ARK5 Using a Novel Kinase Inhibitor ON123300 Exerts Potent Anticancer Activity against Multiple Myeloma.

Journal: Cancer research 20160301

Title: Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas.

Journal: Leukemia 20160101

Title: Better Together: Targeted Combination Therapies in Breast Cancer.

Journal: Seminars in oncology 20151201

Title: FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20151101

Title: Enhancing Endocrine Therapy for Hormone Receptor-Positive Advanced Breast Cancer: Cotargeting Signaling Pathways.

Journal: Journal of the National Cancer Institute 20151001

Title: Brain Exposure of Two Selective Dual CDK4 and CDK6 Inhibitors and the Antitumor Activity of CDK4 and CDK6 Inhibition in Combination with Temozolomide in an Intracranial Glioblastoma Xenograft.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20150901

Title: Palbociclib in Hormone-Receptor-Positive Advanced Breast Cancer.

Journal: The New England journal of medicine 20150716

Title: Palbociclib Extends Survival in Advanced Breast Cancer.

Journal: Cancer discovery 20150701

Title: Phase 2 trial of the cyclin-dependent kinase 4/6 inhibitor palbociclib in patients with retinoblastoma protein-expressing germ cell tumors.

Journal: Cancer 20150501

Title: Palbociclib: first global approval.

Journal: Drugs 20150401

Title: CDK 4/6 inhibitor palbociclib (PD0332991) in Rb+ advanced breast cancer: phase II activity, safety, and predictive biomarker assessment.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20150301

Title: The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study.

Journal: The Lancet. Oncology 20150101

Title: CDK4/6 and IGF1 receptor inhibitors synergize to suppress the growth of p16INK4A-deficient pancreatic cancers.

Journal: Cancer research 20140715

Title: Loss of CDKN2A expression is a frequent event in primary invasive melanoma and correlates with sensitivity to the CDK4/6 inhibitor PD0332991 in melanoma cell lines.

Journal: Pigment cell & melanoma research 20140701

Title: CDK4/6 inhibition provides a potent adjunct to Her2-targeted therapies in preclinical breast cancer models.

Journal: Genes & cancer 20140701

Title: Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia.

Journal: Molecular cancer therapeutics 20140401

Title: MLL fusion-driven activation of CDK6 potentiates proliferation in MLL-rearranged infant ALL.

Journal: Cell cycle (Georgetown, Tex.) 20140301

Title: Synergism of cyclin-dependent kinase inhibitors with camptothecin derivatives in small cell lung cancer cell lines.

Journal: Molecules (Basel, Switzerland) 20140217

Title: [Effect of PD0332991 on biological activity of hematopoietic stem cells in mice].

Journal: Zhonghua xue ye xue za zhi = Zhonghua xueyexue zazhi 20140201

Title: Targeting cell cycle and hormone receptor pathways in cancer.

Journal: Oncogene 20131128

Title: Fulvestrant induces resistance by modulating GPER and CDK6 expression: implication of methyltransferases, deacetylases and the hSWI/SNF chromatin remodelling complex.

Journal: British journal of cancer 20131112

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: PD-0332991, a potent and selective inhibitor of cyclin-dependent kinase 4/6, demonstrates inhibition of proliferation in renal cell carcinoma at nanomolar concentrations and molecular markers predict for sensitivity.

Journal: Anticancer research 20130801

Title: A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS.

Journal: Cancer biology & therapy 20130701

Title: Induction of prolonged early G1 arrest by CDK4/CDK6 inhibition reprograms lymphoma cells for durable PI3Kδ inhibition through PIK3IP1.

Journal: Cell cycle (Georgetown, Tex.) 20130615

Title: Phase II trial of the CDK4 inhibitor PD0332991 in patients with advanced CDK4-amplified well-differentiated or dedifferentiated liposarcoma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20130601

Title: Inhibition of cyclin-dependent kinase 6 suppresses cell proliferation and enhances radiation sensitivity in medulloblastoma cells.

Journal: Journal of neuro-oncology 20130101

Title: PD-0332991, a CDK4/6 inhibitor, significantly prolongs survival in a genetically engineered mouse model of brainstem glioma.

Journal: PloS one 20130101

Title: The requirement for cyclin D function in tumor maintenance.

Journal: Cancer cell 20121016

Title: Therapeutic targeting of the cyclin D3:CDK4/6 complex in T cell leukemia.

Journal: Cancer cell 20121016

Title: Cdk4/6 inhibition induces epithelial-mesenchymal transition and enhances invasiveness in pancreatic cancer cells.

Journal: Molecular cancer therapeutics 20121001

Title: Attenuation of the retinoblastoma pathway in pancreatic neuroendocrine tumors due to increased cdk4/cdk6.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120901

Title: CDK4/6 inhibition antagonizes the cytotoxic response to anthracycline therapy.

Journal: Cell cycle (Georgetown, Tex.) 20120715

Title: Therapeutic response to CDK4/6 inhibition in breast cancer defined by ex vivo analyses of human tumors.

Journal: Cell cycle (Georgetown, Tex.) 20120715

Title: p16-Cdk4-Rb axis controls sensitivity to a cyclin-dependent kinase inhibitor PD0332991 in glioblastoma xenograft cells.

Journal: Neuro-oncology 20120701

Title: The CDK4/6 inhibitor PD0332991 reverses epithelial dysplasia associated with abnormal activation of the cyclin-CDK-Rb pathway.

Journal: Cancer prevention research (Philadelphia, Pa.) 20120601

Title: Selective CDK4/6 inhibition with tumor responses by PD0332991 in patients with mantle cell lymphoma.

Journal: Blood 20120517

Title: An experimental xenograft mouse model of diffuse pontine glioma designed for therapeutic testing.

Journal: Journal of neuro-oncology 20120501

Title: Discovery pharmacokinetic studies in mice using serial microsampling, dried blood spots and microbore LC-MS/MS.

Journal: Bioanalysis 20120501

Title: Multiple roles of cyclin-dependent kinase 4/6 inhibitors in cancer therapy.

Journal: Journal of the National Cancer Institute 20120321

Title: [(18)F]FLT-PET imaging does not always 'light up' proliferating tumor cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120301

Title: Phase I, dose-escalation trial of the oral cyclin-dependent kinase 4/6 inhibitor PD 0332991, administered using a 21-day schedule in patients with advanced cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120115

Title: A systematic screen for CDK4/6 substrates links FOXM1 phosphorylation to senescence suppression in cancer cells.

Journal: Cancer cell 20111115

Title: Retinoblastoma protein modulates the inverse relationship between cellular proliferation and elastogenesis.

Journal: The Journal of biological chemistry 20111021

Title: Quantitative analysis of PD 0332991 in mouse plasma using automated micro-sample processing and microbore liquid chromatography coupled with tandem mass spectrometry.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20111001

Title: Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression.

Journal: Biochemical and biophysical research communications 20110916

Title: Forced expression of cyclin-dependent kinase 6 confers resistance of pro-B acute lymphocytic leukemia to Gleevec treatment.

Journal: Molecular and cellular biology 20110701

Title: Early G₁ cyclin-dependent kinases as prognostic markers and potential therapeutic targets in esophageal adenocarcinoma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110701

Title: Phase I study of PD 0332991, a cyclin-dependent kinase inhibitor, administered in 3-week cycles (Schedule 2/1).

Journal: British journal of cancer 20110607

Title: Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer.

Journal: Endocrine-related cancer 20110601

Title: A bioinformatical and functional approach to identify novel strategies for chemoprevention of colorectal cancer.

Journal: Oncogene 20110428

Title: Expression of p16 and retinoblastoma determines response to CDK4/6 inhibition in ovarian cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110315

Title: [CDK4, a specific target in the treatment of lung adenocarcinomas mutated for KRAS].

Journal: Medecine sciences : M/S 20101201

Title: Quantitative analysis of PD 0332991 in xenograft mouse tumor tissue by a 96-well supported liquid extraction format and liquid chromatography/mass spectrometry.

Journal: Journal of pharmaceutical and biomedical analysis 20101102

Title: RB-pathway disruption in breast cancer: differential association with disease subtypes, disease-specific prognosis and therapeutic response.

Journal: Cell cycle (Georgetown, Tex.) 20101015

Title: Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.

Journal: Journal of medicinal chemistry 20101014

Title: Therapeutic CDK4/6 inhibition in breast cancer: key mechanisms of response and failure.

Journal: Oncogene 20100715

Title: A synthetic lethal interaction between K-Ras oncogenes and Cdk4 unveils a therapeutic strategy for non-small cell lung carcinoma.

Journal: Cancer cell 20100713

Title: Pattern of retinoblastoma pathway inactivation dictates response to CDK4/6 inhibition in GBM.

Journal: Proceedings of the National Academy of Sciences of the United States of America 20100622

Title: Proliferative suppression by CDK4/6 inhibition: complex function of the retinoblastoma pathway in liver tissue and hepatoma cells.

Journal: Gastroenterology 20100501

Title: Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts.

Journal: Cancer research 20100415

Title: The landscape of somatic copy-number alteration across human cancers.

Journal: Nature 20100218

Title: Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors.

Journal: European journal of medicinal chemistry 20100201

Title: Epigenetic silencing of the tumor suppressor microRNA Hsa-miR-124a regulates CDK6 expression and confers a poor prognosis in acute lymphoblastic leukemia.

Journal: Cancer research 20090515

Title: Stem cell factor and interleukin-2/15 combine to enhance MAPK-mediated proliferation of human natural killer cells.

Journal: Blood 20090319

Title: Treatment of growing teratoma syndrome.

Journal: The New England journal of medicine 20090122

Title: Advancing bioluminescence imaging technology for the evaluation of anticancer agents in the MDA-MB-435-HAL-Luc mammary fat pad and subrenal capsule tumor models.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090101

Title: 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.

Journal: Breast cancer research : BCR 20090101

Title: CDK inhibitors as potential breast cancer therapeutics: new evidence for enhanced efficacy in ER+ disease.

Journal: Breast cancer research : BCR 20090101

Title: A novel therapeutic combination using PD 0332991 and bortezomib: study in the 5T33MM myeloma model.

Journal: Cancer research 20080715

Title: Pharmacologic inhibition of CDK4/6: mechanistic evidence for selective activity or acquired resistance in acute myeloid leukemia.

Journal: Blood 20070915

Title: Expression of p16Ink4a compensates for p18Ink4c loss in cyclin-dependent kinase 4/6-dependent tumors and tissues.

Journal: Cancer research 20070515

Title: Mantle cell lymphoma cells express predominantly cyclin D1a isoform and are highly sensitive to selective inhibition of CDK4 kinase activity.

Journal: Blood 20060901

Title: A novel orally active small molecule potently induces G1 arrest in primary myeloma cells and prevents tumor growth by specific inhibition of cyclin-dependent kinase 4/6.

Journal: Cancer research 20060801

Title: Toward understanding the structural basis of cyclin-dependent kinase 6 specific inhibition.

Journal: Journal of medicinal chemistry 20060629

Title: Pharmacologic inhibition of cyclin-dependent kinase 4/6 activity arrests proliferation in myoblasts and rhabdomyosarcoma-derived cells.

Journal: Molecular cancer therapeutics 20060501

Title: Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors.

Journal: Current opinion in pharmacology 20050801

Title: Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.

Journal: Journal of medicinal chemistry 20050407

Title: Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts.

Journal: Molecular cancer therapeutics 20041101

Title: Primary care pediatrics vs. family practice: a nonissue.

Journal: Israel journal of medical sciences 19830801

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Tags:571190-30-2 Molecular Formula|571190-30-2 MDL|571190-30-2 SMILES|571190-30-2 Pd-0332991