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CAS No.: 779353-01-4
Synonyms: SCH 727965;PS-095760
Dinaciclib is a potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.
生物活性
靶点 | CDK1 IC50:3nM | CDK2 IC50:1nM | CDK5 IC50:1nM | Cdk9 IC50:4nM |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|---|---|---|---|---|
NCT00871910 | Solid Tumors ... more >>Lymphoma, Non-Hodgkin Multiple Myeloma Collapse << | Phase 1 | Completed | - | - |
NCT00871546 | Lymphoma, Mantle-Cell ... more >> Leukemia, Lymphocytic, Chronic, B-Cell Collapse << | Phase 2 | Terminated | - | - |
NCT00798213 | Leukemia, Myeloid, Acute ... more >> Lymphoblastic Leukemia, Acute Collapse << | Phase 2 | Terminated | - | - |
实验方案
技术信息
CAS号 | 779353-01-4 | 储存条件 |
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分子式 | C21H28N6O2 | 运输 | 蓝冰 | |||||||||||||
分子量 | 396.49 | 别名 | SCH 727965;PS-095760 | |||||||||||||
溶解度 |
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动物实验配方 |
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Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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1205Lu | 10/30 nM | Growth Inhibition Assay | 72 h | inhibits cell growth and survival | 23527225 |
8226 | 2/5/10 nM | Function Assay | 4 h | blocks induction of XBP-1s and downstream targets | 24362465 |
BaF3/Bcr-abl | 1.5/3/8 nM | Function Assay | 6 h | blocks induction of XBP-1s and downstream targets | 24362465 |
BT-12 | - | Growth Inhibition Assay | - | IC50=8.5 nM | 22315240 |
CA46 | 100 nM | Apoptosis Assay | 24 h | induces cell cycle arrest | 25289887 |
CCRF-CEM | - | Growth Inhibition Assay | - | IC50=5.6 nM | 22315240 |
CHLA-10 | - | Growth Inhibition Assay | - | IC50=6.3 nM | 22315240 |
CHLA-136 | - | Growth Inhibition Assay | - | IC50=9.8 nM | 22315240 |
CHLA-258 | - | Growth Inhibition Assay | - | IC50=9.9 nM | 22315240 |
CHLA-266 | - | Growth Inhibition Assay | - | IC50=7.3 nM | 22315240 |
CHLA-9 | - | Growth Inhibition Assay | - | IC50=8 nM | 22315240 |
CHLA-90 | - | Growth Inhibition Assay | - | IC50=7.5 nM | 22315240 |
COG-LL-317 | - | Growth Inhibition Assay | - | IC50=6.5 nM | 22315240 |
GBM2 | - | Growth Inhibition Assay | - | IC50=6.5 nM | 22315240 |
H929 | 2/5/10 nM | Function Assay | 4 h | blocks induction of XBP-1s and downstream targets | 24362465 |
K562 | 1.5/3/8 nM | Function Assay | 6 h | blocks induction of XBP-1s and downstream targets | 24362465 |
Karpas-299 | - | Growth Inhibition Assay | - | IC50=3.9 nM | 22315240 |
Kasumi-1 | 100 nM | Apoptosis Assay | 24 h | induces cell cycle arrest | 25289887 |
Kasumi-1 | - | Growth Inhibition Assay | - | IC50=4.5 nM | 22315240 |
MIAPaCa-2 | - | Growth Inhibition Assay | 72 h | GI50=10 nM | 21768779 |
ML-1 | 1-1000 nM | Apoptosis Assay | 4 h | induces apoptosis slightly | 21768777 |
MOLT-4 | - | Growth Inhibition Assay | - | IC50=9.3 nM | 22315240 |
NALM-6 | - | Growth Inhibition Assay | - | IC50=4.6 nM | 22315240 |
NB-1643 | - | Growth Inhibition Assay | - | IC50=3.3 nM | 22315240 |
NB-EBc1 | - | Growth Inhibition Assay | - | IC50=7 nM | 22315240 |
Pa20C | - | Growth Inhibition Assay | 72 h | GI50=20 nM | 21768779 |
Ramos-RA1 | - | Growth Inhibition Assay | - | IC50=7.9 nM | 22315240 |
RD | - | Growth Inhibition Assay | - | IC50=8.2 nM | 22315240 |
Rh18 | - | Growth Inhibition Assay | - | IC50=10.5 nM | 22315240 |
Rh30 | - | Growth Inhibition Assay | - | IC50=9 nM | 22315240 |
Rh41 | - | Growth Inhibition Assay | - | IC50=10.5 nM | 22315240 |
RS4;11 | - | Growth Inhibition Assay | - | IC50=5.1 nM | 22315240 |
TC-71 | - | Growth Inhibition Assay | - | IC50=3.9 nM | 22315240 |
U937 | 2/5/10 nM | Function Assay | 3 h | blocks induction of XBP-1s and downstream targets | 24362465 |
U937 | 2/10 nM | Function Assay | 3 h | blocks induction of XBP-1s and downstream targets | 24362465 |
WM1366 | 10/30 nM | Growth Inhibition Assay | 72 h | inhibits cell growth and survival | 23527225 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
---|
NCT00871910 | Solid Tumors ... more >>Lymphoma, Non-Hodgkin Multiple Myeloma Collapse << | Phase 1 | Completed | - | - |
NCT00871546 | Lymphoma, Mantle-Cell ... more >> Leukemia, Lymphocytic, Chronic, B-Cell Collapse << | Phase 2 | Terminated | - | - |
NCT00798213 | Leukemia, Myeloid, Acute ... more >> Lymphoblastic Leukemia, Acute Collapse << | Phase 2 | Terminated | - | - |
NCT01096342 | Refractory Multiple Myeloma | Phase 2 | Completed | - | United States, Arizona ... more >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Florida Mayo Clinic in Florida Jacksonville, Florida, United States, 32224-9980 United States, Michigan Wayne State University/Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Singapore National University Hospital Singapore, Singapore, 119074 Collapse << |
NCT00732810 | Breast Neoplasms ... more >> Carcinoma, Non-Small-Cell Lung Collapse << | Phase 2 | Completed | - | - |
NCT00871663 | Solid Tumors ... more >>Lymphoma, Non-Hodgkin Multiple Myeloma Leukemia, Lymphocytic, Chronic. B-Cell Collapse << | Phase 1 | Completed | - | - |
NCT01096342 | - | - | Completed | - | - |
NCT00937937 | Acral Lentiginous Melanoma ... more >> Lentigo Maligna Melanoma Mucosal Melanoma Nodular Melanoma Recurrent Melanoma Stage IV Cutaneous Melanoma AJCC v6 and v7 Superficial Spreading Melanoma Collapse << | Phase 2 | Active, not recruiting | - | - |
NCT01026324 | Stage IIIB Melanoma ... more >> Stage IIIC Melanoma Stage IV Melanoma Collapse << | Phase 1 Phase 2 | Terminated(Slow accrual) | - | United States, Massachusetts ... more >> Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Collapse << |
NCT00937937 | - | - | Active, not recruiting | - | - |
NCT01026324 | - | - | Terminated(Slow accrual) | - | - |
NCT01580228 | Chronic Lymphocytic Leukemia (... more >>CLL) Collapse << | Phase 3 | Completed | - | - |
NCT01515176 | - | - | Completed | - | - |
NCT01515176 | Chronic Lymphocytic Leukemia ... more >> Prolymphocytic Leukemia Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia Collapse << | Phase 1 Phase 2 | Completed | - | United States, Ohio ... more >> Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 Collapse << |
NCT01434316 | Advanced Malignant Solid Neopl... more >>asm BRCA1 Gene Mutation BRCA2 Gene Mutation Collapse << | Phase 1 | Recruiting | - | United States, Massachusetts ... more >> Massachusetts General Hospital Cancer Center Recruiting Boston, Massachusetts, United States, 02114 Contact: Geoffrey I. Shapiro 617-632-4942 geoffrey_shapiro@dfci.harvard.edu Principal Investigator: Geoffrey I. Shapiro Brigham and Women's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Scott J. Rodig 617-525-7825 srodig@partners.org Principal Investigator: Scott J. Rodig Beth Israel Deaconess Medical Center Recruiting Boston, Massachusetts, United States, 02215 Contact: Gerburg M. Wulf 617-667-9925 Sub-Investigator: Gerburg M. Wulf Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Geoffrey I. Shapiro 617-632-4942 geoffrey_shapiro@dfci.harvard.edu Principal Investigator: Geoffrey I. Shapiro Massachusetts General Hospital Recruiting Charlestown, Massachusetts, United States, 02129 Contact: Jeffrey Supko 617-724-1970 jsupko@partners.org Principal Investigator: Jeffrey Supko Collapse << |
NCT01783171 | Pancreatic Adenocarcinoma ... more >> Recurrent Pancreatic Carcinoma Stage III Pancreatic Cancer AJCC v6 and v7 Stage IV Pancreatic Cancer AJCC v6 and v7 Unresectable Pancreatic Carcinoma Collapse << | Phase 1 | Completed | - | United States, Colorado ... more >> University of Colorado Cancer Center - Anschutz Cancer Pavilion Aurora, Colorado, United States, 80045 University of Colorado Denver, Colorado, United States, 80217-3364 United States, Maryland Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21287 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Canada, Ontario University Health Network-Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Collapse << |
NCT01624441 | Estrogen Receptor Negative ... more >> HER2/Neu Negative Male Breast Carcinoma Progesterone Receptor Negative Recurrent Breast Carcinoma Stage IV Breast Cancer AJCC v6 and v7 Triple-Negative Breast Carcinoma Collapse << | Phase 1 | Completed | - | United States, Texas ... more >> M D Anderson Cancer Center Houston, Texas, United States, 77030 Collapse << |
NCT01711528 | Recurrent Plasma Cell Myeloma | Phase 1 | Completed | - | United States, Arizona ... more >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 United States, Virginia Virginia Commonwealth University/Massey Cancer Center Richmond, Virginia, United States, 23298 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Aspirus UW Cancer Center Wisconsin Rapids, Wisconsin, United States, 54494 Collapse << |
NCT01650727 | Chronic Lymphocytic Leukemia ... more >> Small Lymphocytic Lymphoma Collapse << | Phase 1 | Completed | - | - |
NCT02684617 | rrCLL rrMM ... more >> rrDLBCL Collapse << | Phase 1 | Recruiting | February 6, 2020 | United States, California ... more >> Call for Information (Investigational Site 0024) Recruiting Duarte, California, United States, 91010 Call for Information (Investigational Site 0036) Recruiting Los Angeles, California, United States, 90033 United States, Michigan Call for Information (Investigational Site 0014) Recruiting Detroit, Michigan, United States, 48201 Call for Information (Investigational Site 0028) Recruiting Detroit, Michigan, United States, 48202 United States, Minnesota Call for Information (Investigational Site 0006) Recruiting Rochester, Minnesota, United States, 55905 United States, New Jersey Call for Information (Investigational Site 0003) Recruiting New Brunswick, New Jersey, United States, 08903 United States, New York Call for Information (Investigational Site 0026) Recruiting Buffalo, New York, United States, 14263 United States, Ohio Call for Information (Investigational Site 0002) Recruiting Columbus, Ohio, United States, 43210 United States, Pennsylvania Call for Information (Investigational Site 0023) Recruiting Hershey, Pennsylvania, United States, 17033 United States, Texas Call for Information (Investigational Site 0017) Recruiting Dallas, Texas, United States, 75246 United States, Washington Call for Information (Investigational Site 0011) Recruiting Seattle, Washington, United States, 98116 United States, Wisconsin Call for Information (Investigational Site 0018) Recruiting Madison, Wisconsin, United States, 53792 Australia Merck Sharp & Dohme Recruiting North Ryde, Australia Contact: Australian Medical Information Centre 61 2 8988 8428 Collapse << |
NCT03484520 | Acute Myeloid Leukemia (AML) | Phase 1 | Recruiting | June 2, 2021 | United States, Arizona ... more >> Mayo Clinic Arizona /ID# 201705 Not yet recruiting Phoenix, Arizona, United States, 85054 United States, Arkansas University of Arkansas /ID# 200016 Not yet recruiting Little Rock, Arkansas, United States, 72205 United States, California Cedars-Sinai Medical Ctr /ID# 202245 Not yet recruiting Los Angeles, California, United States, 90048 David Geffen School of Medicin /ID# 200015 Not yet recruiting Los Angeles, California, United States, 90095 United States, Illinois The University of Chicago /ID# 200017 Recruiting Chicago, Illinois, United States, 60637 United States, Maryland Univ Maryland School Medicine /ID# 204015 Not yet recruiting Baltimore, Maryland, United States, 21201 United States, North Carolina Wake Forest Baptist Medical Center /ID# 200288 Not yet recruiting Winston-Salem, North Carolina, United States, 27157-0001 United States, Ohio The Ohio State University - Columbus /ID# 200668 Not yet recruiting Columbus, Ohio, United States, 43210 United States, Texas Univ TX, MD Anderson /ID# 205215 Not yet recruiting Houston, Texas, United States, 77030 Australia, Queensland Gold Coast University Hospital /ID# 202759 Not yet recruiting Southport, Queensland, Australia, 4215 Australia, Tasmania Royal Hobart Hospital /ID# 202763 Not yet recruiting Hobart, Tasmania, Australia, 7000 Australia, Victoria Monash Medical Centre /ID# 202762 Not yet recruiting Melbourne, Victoria, Australia, 3168 Spain Hospital Universitario y Politecnico La Fe /ID# 202318 Recruiting Valencia, Valenciana, Spain, 46026 Hospital Ramon y Cajal /ID# 201729 Recruiting Madrid, Spain, 28036 Hospital Clinico Univ de Salamanca /ID# 201728 Recruiting Salamanca, Spain, 37007 Collapse << |
NCT01676753 | Advanced or Metastatic Breast ... more >>Cancer Triple Negative Breast Cancer Collapse << | Phase 1 | Recruiting | August 2019 | United States, California ... more >> UCSF Helen Diller Family Comprehensive Cancer Center Recruiting San Francisco, California, United States, 94143 Contact: A. Jo Chien, MD 877-827-3222 cancertrials@ucsf.edu Principal Investigator: A. Jo Chien, MD Principal Investigator: Andrei Goga, MD, PhD Sub-Investigator: Michelle Melisko, MD Sub-Investigator: Mark Moasser, MD Sub-Investigator: Pamela N Munster, MD Sub-Investigator: Hope Rugo, MD Sub-Investigator: John Park, MD Sub-Investigator: Melanie Majure, MD Collapse << |
靶点 | Description | IC50 |
---|---|---|
CDK1 | IC50:3nM | |
CDK2 | IC50:1nM | |
CDK5 | IC50:1nM | |
Cdk9 | IC50:4nM |
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