Flavopiridol Hydrochloride
Based on 54 publication(s) in Google Scholar
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 131740-09-5
- Formula: C21H21Cl2NO5
- Molecular Weight:438.30
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Flavopiridol Hydrochloride
More- Nature. 2025 Aug;644(8076):557-566. [Abstract]
- Nature. 2024 Apr;628(8007):408-415. [Abstract]
- Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]
- Cancer Discov. 2021 Oct 6;candisc.1848.2020. [Abstract]
- Nat Biomed Eng. 2025 Oct 16. [Abstract]
- Nat Commun. 2024 Dec 5;15(1):10594. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2022 Jul;12(7):3139-3155. [Abstract]
- Biomaterials. 2014 Aug;35(24):6585-94. [Abstract]
- Plant Cell. 2025 Apr 2;37(4):koaf071. [Abstract]
- Int J Biol Sci. 2023 Aug 6;19(13):4123-4138. [Abstract]
- Cell Commun Signal. 2022 Sep 5;20(1):96. [Abstract]
- Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. [Abstract]
- Proc Natl Acad Sci U S A. 2021 Nov 16;118(46):e2115667118. [Abstract]
- Cell Chem Biol. 2019 Aug 15;26(8):1067-1080.e8. [Abstract]
- Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. [Abstract]
- Int J Biol Macromol. 2025 Jun;315(Pt 1):144179. [Abstract]
- EMBO Mol Med. 2025 Nov 26. [Abstract]
- Cell Rep. 2020 Apr 28;31(4):107586. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cell Mol Life Sci. 2021 Feb;78(3):949-962. [Abstract]
- EMBO Rep. 2022 Jun 7;23(6):e53932. [Abstract]
- Am J Physiol Cell Physiol. 2025 Aug 20. [Abstract]
- ACS Omega. 2025 Aug 16;10(33):38240-38254. [Abstract]
- Molecules. 2023 Mar 4;28(5):2368. [Abstract]
- Sci Rep. 2024 Oct 31;14(1):26239. [Abstract]
- Sci Rep. 2021 Mar 8;11(1):5374. [Abstract]
- Sci Rep. 2015 Dec 1:5:17675. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- J Virol. 2026 May 11.
- PLoS Genet. 2024 Jun 3;20(6):e1011308. [Abstract]
- Int J Med Sci. 2025 Jan 27;22(4):940-954. [Abstract]
- ACS Chem Biol. 2017 May 19;12(5):1245-1256. [Abstract]
- Toxicol Lett. 2024 Nov:401:44-54. [Abstract]
- Biochem Biophys Res Commun. 2019 Jun 11;513(4):967-973. [Abstract]
- Turk Neurosurg. 2016;26(6):922-929. [Abstract]
- Albert Einstein College of Medicine. 2026.
- bioRxiv. 2025 Oct 9:2025.10.08.680157. [Abstract]
- bioRxiv. 2025 Aug 19.
- University of Washington. 2025.
- bioRxiv. 2024 Sep 29:2024.09.28.615444. [Abstract]
- bioRxiv. 2024 July 27.
- Research Square Preprint. 2024 May 2.
- Research Square Preprint. 2024 Apr 2.
- bioRxiv. 2024 Mar 17.
- bioRxiv. 2023 Sep 7.
- Purdue University. 2022.
- The University of Chicago. 2022 Aug.
- Research Square Preprint. 2022 Jan.
- Free University of Berlin. 2021 Mar.
- University of North Carolina at Chapel Hill. 2020 Jun.
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Cell Imaging/Staining
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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IHC
Biological Activity
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CDK1/Cyc B1 30 nM (IC50) |
CDK2/Cyc E 170 nM (IC50) |
CDK4/Cyc D1 100 nM (IC50) |
MAP 19000 nM (IC50) |
PKC 14000 nM (IC50) |
EGFR 22000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
0.06 μM
Compound: ALVOCIDIB
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
|
10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
0.59 μM
Compound: ALVOCIDIB
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
|
10.21203/rs.3.rs-23951/v1 |
Flavopiridol (2 μM) robustly induces a distinct pattern of ER stress in CLL cells that contributes to cell death through IRE1-mediated activation of ASK1 and possibly downstream caspases[1]. Flavopiridol results in potent upregulation of a number of PRGs in treatments lasting 4-24 h. Flavopiridol has and immediate and long-term effect on the expression of several PRGs. In serum starved cells re-stimulated with serum, flavopiridol also inhibits the expression of these genes, but subsequently, JUNB, GADD45B and EGR1 are upregulated in the presence of flavopiridol[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 131740-09-5
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Appearance Solid
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Molecular Weight 438.30
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Formula C21H21Cl2NO5
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Color Light yellow to khaki
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SMILES
O=C1C2=C(C=C(C([C@]3([H])[C@H](O)CN(C)CC3)=C2OC(C4=CC=CC=C4Cl)=C1)O)O.[H]Cl
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Synonyms
Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (54)
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Journal Impact Factor
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Most Recent
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Nature
2025 Aug;644(8076):557-566. PMID: 40604277
Flavopiridol Hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Aug;644(8076):557-566. [Abstract]
Nucleolar morphology (IF for RPA194, FBL, and NPM1 for FC, DFC and GC) in DMSO (-FVP) and after 30-90 min of 2 μM FVP (Flavopiridol) treatment.
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Nature
2024 Apr;628(8007):408-415. PMID: 38480883
Flavopiridol Hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2024 Apr;628(8007):408-415. [Abstract]
Immunoblotting showing CDK9, Ser2P and β-Actin protein levels in macrophages treated with either DMSO or Flavopiridol (10 μM) for 30 min. n = 3 independent experiments.
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Cell
2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809 -
Cancer Discov
Transcription Elongation Machinery Is a Druggable Dependency and Potentiates Immunotherapy in Glioblastoma Stem Cells. [Abstract]2021 Oct 6;candisc.1848.2020. PMID: 34615656 -
Nat Biomed Eng
Inhibition of LARP4-mediated quiescence exit of naive CD4+ T cells ameliorates autoimmune and allergic diseases. [Abstract]2025 Oct 16. PMID: 41102557 -
Nat Commun
CDK9 recruits HUWE1 to degrade RARα and offers therapeutic opportunities for cutaneous T-cell lymphoma. [Abstract]2024 Dec 5;15(1):10594. PMID: 39632829 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Acta Pharm Sin B
Engineering prodrug nanomicelles as pyroptosis inducer for codelivery of PI3K/mTOR and CDK inhibitors to enhance antitumor immunity. [Abstract]2022 Jul;12(7):3139-3155. PMID: 35865097
Flavopiridol Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Jul;12(7):3139-3155. [Abstract]
Flavopiridol (Flav; 0-1 μg/mL; 24 h). MTT assay-derived curves of PF, Flav, PF + Flav and PNM in 4T1 cells after 24 h of treatment.
Flavopiridol Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Jul;12(7):3139-3155. [Abstract]
Flavopiridol (Flav; 5 mg/kg; i.v.). Schedule of establishment of the 4T1 tumor-bearing mouse model and different treatments. Average tumor growth curves of the mice treated with PBS, PF, Flav, PF + Flav and PNM.
Flavopiridol Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Jul;12(7):3139-3155. [Abstract]
Flavopiridol (Flav; 5 mg/kg; i.v.). Representative pictures of HE staining and Ki-67 staining in tumor sections of different groups.
Flavopiridol Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2022 Jul;12(7):3139-3155. [Abstract]
Flavopiridol (Flav; 5 mg/kg; i.v.). Representative flow cytometric plots of CD8+ T cells in tumors.
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Biomaterials
Repair of spinal cord injury by inhibition of astrocyte growth and inflammatory factor synthesis through local delivery of flavopiridol in PLGA nanoparticles. [Abstract]2014 Aug;35(24):6585-94. PMID: 24811262 -
Plant Cell
ZmSSRP1 facilitates the progression of RNA polymerase II and is essential for kernel development in maize. [Abstract]2025 Apr 2;37(4):koaf071. PMID: 40166832 -
Int J Biol Sci
DDX24 Mutation Alters NPM1 Phase Behavior and Disrupts Nucleolar Homeostasis in Vascular Malformations. [Abstract]2023 Aug 6;19(13):4123-4138. PMID: 37705750 -
Cell Commun Signal
Elevation of effective p53 expression sensitizes wild-type p53 breast cancer cells to CDK7 inhibitor THZ1. [Abstract]2022 Sep 5;20(1):96. PMID: 36058938 -
Clin Cancer Res
Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]2020 Apr 15;26(8):2011-2021. PMID: 31937620 -
Proc Natl Acad Sci U S A
Cell division in the shoot apical meristem is a trigger for miR156 decline and vegetative phase transition in Arabidopsis. [Abstract]2021 Nov 16;118(46):e2115667118. PMID: 34750273 -
Cell Chem Biol
Multiomics Profiling Establishes the Polypharmacology of FDA-Approved CDK4/6 Inhibitors and the Potential for Differential Clinical Activity. [Abstract]2019 Aug 15;26(8):1067-1080.e8. PMID: 31178407 -
Cell Chem Biol
2018 Feb 15;25(2):135-142.e5. PMID: 29276047 -
Int J Biol Macromol
Trained immunity driven by Enterococcus faecalis ribosomal protein S11 enhances antigen presentation and boosts influenza vaccine efficacy via nanoparticle delivery. [Abstract]2025 Jun;315(Pt 1):144179. PMID: 40381785 -
EMBO Mol Med
Isomeranzin activates Gnas-AMPK signaling to drive white adipose browning and curb obesity in mice. [Abstract]2025 Nov 26. PMID: 41299101 -
Cell Rep
2020 Apr 28;31(4):107586. PMID: 32348767 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Cell Mol Life Sci
TGF-β1 promotes epithelial-to-mesenchymal transition and stemness of prostate cancer cells by inducing PCBP1 degradation and alternative splicing of CD44. [Abstract]2021 Feb;78(3):949-962. PMID: 32440711 -
EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787 -
Am J Physiol Cell Physiol
Thrombopoietin Mitigates Neuronal Death by Enhancing Mitophagy and Suppressing NLRP3 Inflammasome Activation Under Oxygen-Glucose Deprivation Conditions. [Abstract]2025 Aug 20. PMID: 40833847 -
ACS Omega
Total Synthesis of Rohitukine and Dysoline and Their Anticancer Analogues Flavopiridol and IIIM-290. [Abstract]2025 Aug 16;10(33):38240-38254. PMID: 40893326 -
Molecules
Development and Validation of a Rapid LC-MS/MS Method for Quantifying Alvocidib: In Silico and In Vitro Metabolic Stability Estimation in Human Liver Microsomes. [Abstract]2023 Mar 4;28(5):2368. PMID: 36903615 -
Sci Rep
Flavopiridol induces cell cycle arrest and apoptosis by interfering with CDK1 signaling pathway in human ovarian granulosa cells. [Abstract]2024 Oct 31;14(1):26239. PMID: 39482384 -
Sci Rep
2021 Mar 8;11(1):5374. PMID: 33686114 -
Sci Rep
2015 Dec 1:5:17675. PMID: 26620302 -
Cancers (Basel)
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]2022 Mar 19;14(6):1575. PMID: 35326726 -
iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
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PLoS Genet
Myeloid Targeted Human MLL-ENL and MLL-AF9 Induces cdk9 and bcl2 Expression in Zebrafish Embryos. [Abstract]2024 Jun 3;20(6):e1011308. PMID: 38829886 -
Int J Med Sci
NCAPH Promotes the Proliferation of Prostate Cancer Cells Via Modulating the E2F1 Mediated PI3K/AKT/mTOR Axis. [Abstract]2025 Jan 27;22(4):940-954. PMID: 39991770 -
ACS Chem Biol
A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family. [Abstract]2017 May 19;12(5):1245-1256. PMID: 28263556 -
Toxicol Lett
Flavopiridol inhibits oocyte maturation, reduces oocyte quality and blocks cumulus cell function. [Abstract]2024 Nov:401:44-54. PMID: 39276810 -
Biochem Biophys Res Commun
2019 Jun 11;513(4):967-973. PMID: 31005255 -
Turk Neurosurg
Intrathecal Administration of Flavopiridol Promotes Regeneration in Experimental Model of Spinal Cord Injury. [Abstract]2016;26(6):922-929. PMID: 27476919 -
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bioRxiv
2025 Oct 9:2025.10.08.680157. PMID: 41279244 -
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bioRxiv
2024 Sep 29:2024.09.28.615444. PMID: 39386460 -
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Solvent & Solubility
DMSO : ≥ 20 mg/mL (45.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 20 mg/mL (45.63 mM)
DMF : 7.69 mg/mL (17.55 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.67 mg/mL (1.53 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.67 mg/mL (1.53 mM); Clear solution
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 5%DMSO 95%(10%Tween80 in Saline)
Solubility: mg/mL; null solution; Need ultrasonic and warming and adjust pH toMSwithMSO
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Briefly, lysates containing approximately 3×106 cells are incubated with 50 μM LEVD-AFC (caspase 4 substrate) or LETD-AFC (caspase 8 substrate) containing 10 mM dithiothretiol (DTT). Caspase 4 activity is measured one hour after addition of substrate and caspase 8 activity is measured 30 minutes after addition of substrate. Release of free AFC is measured with a Beckman-Coulter DTX 880 multimode detector.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The cells treated with flavopiridol are washed after 4 hours with PBS and resuspended in regular growth medium (RPMI 1640) supplemented with 10% human serum and antibiotics for the remainder of the incubation time. In the case of flavopiridol/chloroquine samples, chloroquine is re-added in the fresh media after flavopiridol is washed at 4 hours. For all the other conditions, cells are incubated with the respective drugs for 24 hours continuously.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Mahoney E, et al. ER stress and autophagy: new discoveries in the mechanism of action and drug resistance of the cyclin-dependent kinase inhibitor flavopiridol.Blood. 2012 Aug 9;120(6):1262-1273. [Content Brief]
[2]. Keskin H, et al. Complex effects of flavopiridol on the expression of primary response genes. Cell Div. 2012 Mar 29;7:11. [Content Brief]
[3]. Kim KS, et al.Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. J Med Chem. 2000 Nov 2;43(22):4126-34. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF / DMSO / H2O | 1 mM | 2.2815 mL | 11.4077 mL | 22.8154 mL | 57.0386 mL |
| 5 mM | 0.4563 mL | 2.2815 mL | 4.5631 mL | 11.4077 mL | |
| 10 mM | 0.2282 mL | 1.1408 mL | 2.2815 mL | 5.7039 mL | |
| 15 mM | 0.1521 mL | 0.7605 mL | 1.5210 mL | 3.8026 mL | |
| DMSO / H2O | 20 mM | 0.1141 mL | 0.5704 mL | 1.1408 mL | 2.8519 mL |
| 25 mM | 0.0913 mL | 0.4563 mL | 0.9126 mL | 2.2815 mL | |
| 30 mM | 0.0761 mL | 0.3803 mL | 0.7605 mL | 1.9013 mL | |
| 40 mM | 0.0570 mL | 0.2852 mL | 0.5704 mL | 1.4260 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.