Structure of Flavopiridol HCl
CAS No.: 131740-09-5
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad-spectrum CDK inhibitor that competes with ATP to inhibit CDKs including CDK1, CDK2, and CDK4, with IC50 values of 30 nM, 170 nM, and 100 nM, respectively.
Synonyms: HMR-1275 Hydrochloride; L86-8275 Hydrochloride; L-868,275
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CAS No. : | 131740-09-5 |
Formula : | C21H21Cl2NO5 |
M.W : | 438.30 |
SMILES Code : | O=C1C=C(C2=CC=CC=C2Cl)OC3=C1C(O)=CC(O)=C3[C@@H]4[C@H](O)CN(C)CC4.[H]Cl |
Synonyms : |
HMR-1275 Hydrochloride; L86-8275 Hydrochloride; L-868,275
|
MDL No. : | MFCD26792554 |
InChI Key : | LGMSNQNWOCSPIK-LWHGMNCYSA-N |
Pubchem ID : | 9910986 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
In Vitro:
Concentration | Treated Time | Description | References |
U2OS cells | 2 μM | 90-120 min | To investigate the effect of Flavopiridol on transcription elongation inhibition, results showed that Flavopiridol significantly reduced Pol II elongation activity but did not significantly affect the dynamics of SAGA and ATAC complexes. | PMC5599802 |
HeLa cells | 1 μM | 30 min | To investigate the effect of Flavopiridol on KPNB1 gene transcription, results showed that Flavopiridol effectively inhibited KPNB1 transcription past the poly(A) site. | PMC4424039 |
LNCaP-abl cells | 300 nM | 1 h | FP inhibits CDK9 phosphorylation of RNA Pol II to block the ability of the PIC to transition to the elongation phase of transcription. PAF1 is trapped at the promoter following FP treatment and travels through the gene body over time points after release. | PMC8566496 |
A549 cells | 20μM | 24 h | Inhibited A549 cell proliferation, increased cell apoptosis, and decreased clone formation, migration, and invasion ability | PMC7242448 |
PDX cell lines | 0.1 µM | 24 h | To evaluate the inhibitory effect of Flavopiridol on PDX cell lines, results showed that Flavopiridol significantly inhibited cell proliferation and induced apoptosis. | PMC11185924 |
Normal dermal fibroblasts | 0.1 µM | 24 h | To evaluate the toxicity of Flavopiridol on normal cells, results showed that Flavopiridol had a weak inhibitory effect on normal cells. | PMC11185924 |
Human chondrocytes | 250nM | 5 h | Suppressed IL-1β-induced iNOS gene expression, Flavopiridol alone achieved 100% suppression of iNOS mRNA induction. | PMC7785706 |
Bovine cartilage explants | 60nM | 6 days | Protected cartilage tissue from IL-1β-induced degradation, Flavopiridol combined with JQ1 significantly reduced GAG release. | PMC7785706 |
In Vivo:
Administration | Dosage | Frequency | Description | References |
BALB/c nude mice | Lung cancer xenograft model | Intraperitoneal injection | 8 mg/kg | Three times per week for 41 days | Inhibited tumor growth, reduced tumor volume and weight, and significantly decreased GBE1 expression | PMC7242448 |
Mice | PDX282 tumor model | Intraperitoneal injection | 5 mg/kg | 3 times per week for 11 days | To evaluate the antitumor effect of Flavopiridol in vivo, results showed that Flavopiridol significantly inhibited tumor growth but was accompanied by weight loss and unexpected death. | PMC11185924 |
Mice | ACL rupture model | Intraperitoneal injection | 2.5mg/kg | Immediately after injury, then 3 times per week for up to 4 weeks | Reduced inflammation and PTOA progression after ACL rupture, the combined treatment significantly suppressed IL-1β and IL-6 mRNA expression and reduced synovitis and OARSI scores. | PMC7785706 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT02520011 | Acute Myeloid Leukemia | Phase 2 | Recruiting | December 2019 | - |
NCT00006485 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less << |
NCT00087282 | Liver Cancer | Phase 2 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less << |
NCT00007917 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, Massachusetts ... More >> Massachusetts General Hospital Cancer Center Boston, Massachusetts, United States, 02114 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 Less << |
NCT00634244 | - | Completed | - | - | |
NCT00021073 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, Minnesota ... More >> Mayo Clinic Rochester, Minnesota, United States, 55905 Less << |
NCT00470197 | Adult Acute Megakaryoblastic L... More >>eukemia (M7) Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Malignant Neoplasm Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Less << | Phase 1 | Completed | - | United States, Maryland ... More >> Johns Hopkins University Baltimore, Maryland, United States, 21287-8936 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Less << |
NCT00042874 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT00634244 | Adult Acute Megakaryoblastic L... More >>eukemia (M7) Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Recurrent Adult Acute Myeloid Leukemia Less << | Phase 2 | Completed | - | United States, Alabama ... More >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, Arizona Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Florida Mayo Clinic in Florida Jacksonville, Florida, United States, 32224-9980 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Iowa Siouxland Hematology Oncology Associates Sioux City, Iowa, United States, 51101 United States, Maryland Johns Hopkins University/Sidney Kimmel Comprehensive Cancer Center Baltimore, Maryland, United States, 21287 United States, Massachusetts Tufts Medical Center Boston, Massachusetts, United States, 02111 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Ohio The Jewish Hospital Cincinnati, Ohio, United States, 45236 United States, Pennsylvania Geisinger Medical Center Danville, Pennsylvania, United States, 17822-2001 Geisinger Medical Center-Cancer Center Hazleton Hazleton, Pennsylvania, United States, 18201 Penn State Milton S Hershey Medical Center Hershey, Pennsylvania, United States, 17033-0850 Lewistown Hospital Lewistown, Pennsylvania, United States, 17044 Geisinger Medical Group State College, Pennsylvania, United States, 16801 Mount Nittany Medical Center State College, Pennsylvania, United States, 16803 Geisinger Wyoming Valley Wilkes-Barre, Pennsylvania, United States, 18711 United States, Tennessee Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 United States, Wisconsin University of Wisconsin Hospital and Clinics Madison, Wisconsin, United States, 53792 Froedtert and the Medical College of Wisconsin Milwaukee, Wisconsin, United States, 53226 Israel Rambam Medical Center Haifa, Israel, 31096 Less << |
NCT00407966 | - | Completed | - | - | |
NCT00407966 | Adult Acute Basophilic Leukemi... More >>a Adult Acute Eosinophilic Leukemia Adult Acute Megakaryoblastic Leukemia (M7) Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Secondary Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia Less << | Phase 2 | Completed | - | United States, Maryland ... More >> Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21287 Less << |
NCT00795002 | - | Completed | - | - | |
NCT00795002 | Acute Myeloid Leukemia With Mu... More >>ltilineage Dysplasia Following Myelodysplastic Syndrome Adult Acute Megakaryoblastic Leukemia (M7) Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Del(5q) Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Secondary Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia Less << | Phase 2 | Completed | - | United States, Maryland ... More >> Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21287 United States, Washington Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium Seattle, Washington, United States, 98109 Less << |
NCT00046917 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT01349972 | Acute Myeloid Leukemia With Mu... More >>ltilineage Dysplasia Following Myelodysplastic Syndrome Adult Acute Minimally Differentiated Myeloid Leukemia (M0) Adult Acute Monoblastic Leukemia (M5a) Adult Acute Monocytic Leukemia (M5b) Adult Acute Myeloblastic Leukemia With Maturation (M2) Adult Acute Myeloblastic Leukemia Without Maturation (M1) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities Adult Acute Myeloid Leukemia With Del(5q) Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) Adult Acute Myeloid Leukemia With t(16;16)(p13;q22) Adult Acute Myeloid Leukemia With t(8;21)(q22;q22) Adult Acute Myelomonocytic Leukemia (M4) Adult Erythroleukemia (M6a) Adult Pure Erythroid Leukemia (M6b) Secondary Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia Less << | Phase 2 | Completed | - | United States, Arizona ... More >> Mayo Clinic Scottsdale-Phoenix Scottsdale, Arizona, United States, 85259 United States, Florida Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Georgia Blood and Marrow Transplant Group of Georgia Atlanta, Georgia, United States, 30342 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Maryland University of Maryland/Greenebaum Cancer Center Baltimore, Maryland, United States, 21201 Johns Hopkins University/Sidney Kimmel Comprehensive Cancer Center Baltimore, Maryland, United States, 21287 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Tennessee Vanderbilt-Ingram Cancer Center Nashville, Tennessee, United States, 37232 United States, Texas Baylor University Medical Center Dallas, Texas, United States, 75246 United States, Virginia Virginia Commonwealth University Richmond, Virginia, United States, 23298 Less << |
NCT00079352 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, New Mexico ... More >> University of New Mexico Albuquerque, New Mexico, United States, 87106 Less << |
NCT01349972 | - | Completed | - | - | |
NCT00991952 | - | Completed | - | - | |
NCT00072436 | Unspecified Adult Solid Tumor,... More >> Protocol Specific Less << | Phase 1 | Completed | - | United States, Massachusetts ... More >> Massachusetts General Hospital Cancer Center Boston, Massachusetts, United States, 02114 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT01076556 | Chronic Lymphocytic Leukemia ... More >> Prolymphocytic Leukemia Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia Stage I Chronic Lymphocytic Leukemia Stage I Small Lymphocytic Lymphoma Stage II Chronic Lymphocytic Leukemia Stage II Small Lymphocytic Lymphoma Stage III Chronic Lymphocytic Leukemia Stage III Small Lymphocytic Lymphoma Stage IV Chronic Lymphocytic Leukemia Stage IV Small Lymphocytic Lymphoma Less << | Phase 1 | Terminated | - | United States, Ohio ... More >> Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 Less << |
NCT00991952 | Adenocarcinoma of the Gastroes... More >>ophageal Junction Diffuse Adenocarcinoma of the Stomach Intestinal Adenocarcinoma of the Stomach Mixed Adenocarcinoma of the Stomach Recurrent Gastric Cancer Stage IIIA Gastric Cancer Stage IIIB Gastric Cancer Stage IIIC Gastric Cancer Stage IV Gastric Cancer Less << | Phase 2 | Completed | - | United States, California ... More >> City of Hope Duarte, California, United States, 91010 UC Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Illinois University of Chicago Comprehensive Cancer Center Chicago, Illinois, United States, 60637-1470 United States, Michigan University of Michigan Ann Arbor, Michigan, United States, 48109 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT00735930 | Anemia Chroni... More >>c Lymphocytic Leukemia Prolymphocytic Leukemia Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia Thrombocytopenia Less << | Phase 1 | Completed | - | United States, Ohio ... More >> Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 Less << |
NCT00957905 | Recurrent Extragonadal Seminom... More >>a Recurrent Malignant Extragonadal Germ Cell Tumor Recurrent Malignant Extragonadal Non-Seminomatous Germ Cell Tumor Recurrent Malignant Testicular Germ Cell Tumor Recurrent Ovarian Germ Cell Tumor Stage III Testicular Cancer Stage IV Extragonadal Non-Seminomatous Germ Cell Tumor Stage IV Extragonadal Seminoma Stage IV Ovarian Germ Cell Tumor Less << | Phase 2 | Completed | - | United States, California ... More >> Tower Cancer Research Foundation Beverly Hills, California, United States, 90211-1850 City of Hope Comprehensive Cancer Center Duarte, California, United States, 91010 USC / Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 University of California Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Illinois University of Chicago Comprehensive Cancer Center Chicago, Illinois, United States, 60637 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 United States, Pennsylvania UPMC-Presbyterian Hospital Pittsburgh, Pennsylvania, United States, 15213 University of Pittsburgh Cancer Institute (UPCI) Pittsburgh, Pennsylvania, United States, 15232 United States, Wisconsin Riverview Hospital Wisconsin Rapids, Wisconsin, United States, 54494 Less << |
NCT00082784 | Extranodal Marginal Zone Lymph... More >>oma of Mucosa-Associated Lymphoid Tissue Nodal Marginal Zone Lymphoma Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Adult Diffuse Mixed Cell Lymphoma Recurrent Adult Diffuse Small Cleaved Cell Lymphoma Recurrent Grade 1 Follicular Lymphoma Recurrent Grade 2 Follicular Lymphoma Recurrent Grade 3 Follicular Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Marginal Zone Lymphoma Refractory Plasma Cell Myeloma Splenic Marginal Zone Lymphoma Waldenstrom Macroglobulinemia Less << | Phase 1 | Completed | - | United States, Florida ... More >> Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Pennsylvania University of Pittsburgh Cancer Institute Pittsburgh, Pennsylvania, United States, 15232 University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15232 United States, South Carolina Medical University of South Carolina Charleston, South Carolina, United States, 29425 United States, Virginia Virginia Commonwealth University/Massey Cancer Center Richmond, Virginia, United States, 23298 Less << |
NCT00098579 | Gastrointestinal Stromal Tumor... More >> Recurrent Adult Soft Tissue Sarcoma Stage IV Adult Soft Tissue Sarcoma Less << | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT00047307 | Adenocarcinoma of the Pancreas... More >> Recurrent Pancreatic Cancer Stage II Pancreatic Cancer Stage III Pancreatic Cancer Stage IV Pancreatic Cancer Less << | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 Less << |
NCT00957905 | - | Completed | - | - |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.28mL 0.46mL 0.23mL |
11.41mL 2.28mL 1.14mL |
22.82mL 4.56mL 2.28mL |