Ribociclib succinate
Based on 84 publication(s) in Google Scholar
RRibociclib (LEE011) succinate is an ATP-competitive and orally active CDK4/6 inhibitor that crosses the blood-brain barrier with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 1374639-75-4
- Formel: C27H36N8O5
- Molecular Weight:552.63
-
Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
CNS-Penetrant Compound Library
HY-L028
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Breast Cancer Compound Library
HY-L074
-
Drug-Induced Liver Injury (DILI) Compound Library
HY-L076
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
EMA-Approved Drug Library
HY-L116
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Human Metabolite Library
HY-L123
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Cancer Approved Drug Library
HY-L213
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
-
FDA Kinase Inhibitor Library
HY-L230
-
High-Efficiency Gene Editing Compound Library
HY-L244
Publications Citing Use of MedChemExpress (MCE) Ribociclib succinate
More- Cancer Cell. 2024 Aug 27:S1535-6108(24)00305-2. [Abstract]
- Cell. 2025 Oct 30;188(22):6301-6316.e29. [Abstract]
- Cell. 2023 Jun 8;186(12):2628-2643.e21. [Abstract]
- Cancer Discov. 2024 Mar 1;14(3):446-467. [Abstract]
- Nat Cancer. 2021 Apr;2(4):429-443. [Abstract]
- Mil Med Res. 2022 Dec 19;9(1):71. [Abstract]
- Cancer Res. 2025 Apr 3;85(7):1297-1309. [Abstract]
- Cancer Res. 2019 Oct 15;79(20):5245-5259. [Abstract]
- Mol Cell. 2017 Oct 19;68(2):336-349.e6. [Abstract]
- Nat Commun. 2026 Jun 17;17(1):5361. [Abstract]
- Nat Commun. 2026 Jan 22;17(1):619. [Abstract]
- Nat Commun. 2022 Aug 10;13(1):4689. [Abstract]
- Nat Commun. 2021 Sep 10;12(1):5386. [Abstract]
- Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
- Nat Commun. 2019 Jun 28;10(1):2860. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2022 Dec 23;8(51):eadc8911. [Abstract]
- Cell Rep Med. 2025 Dec 29:102526. [Abstract]
- Cell Rep Med. 2023 Oct 17;4(10):101200. [Abstract]
- Clin Cancer Res. 2025 Mar 3;31(5):907-920. [Abstract]
- Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]
- Cancer Lett. 2026 May 28:646:218429. [Abstract]
- Int J Biol Sci. 2019 Jan 1;15(3):522-532. [Abstract]
- Cell Death Dis. 2020 Sep 15;11(9):754. [Abstract]
- Int J Biol Macromol. 2024 Dec 27:139117. [Abstract]
- NPJ Precis Oncol. 2025 May 27;9(1):156. [Abstract]
- NPJ Precis Oncol. 2021 Mar 19;5(1):20. [Abstract]
- NPJ Breast Cancer. 2025 Dec 3;11(1):135. [Abstract]
- J Transl Med. 2026 Feb 4;24(1):385. [Abstract]
- J Transl Med. 2022 May 13;20(1):217. [Abstract]
- Biomed Pharmacother. 2019 Apr:112:108602. [Abstract]
- Cell Chem Biol. 2025 Apr 17;32(4):556-569.e24. [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]
- Eur J Cancer. 2018 Oct:102:10-22. [Abstract]
- Cell Rep. 2020 Aug 4;32(5):107995. [Abstract]
- Cell Rep. 2017 Oct 31;21(5):1386-1398. [Abstract]
- JCI Insight. 2022 Feb 8;7(3):e154402. [Abstract]
- Int J Mol Med. 2025 Nov;56(5):167. [Abstract]
- Biochem Pharmacol. 2025 Jan 9:116744. [Abstract]
- Breast Cancer Res. 2019 Dec 26;21(1):150. [Abstract]
- Pharmaceutics. 2025 Jul 25;17(8):967. [Abstract]
- Mol Cancer Ther. 2018 May;17(5):897-907. [Abstract]
- Cells. 2026 Feb 28;15(5):430. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- RSC Adv. 2020, 10(38):22668-22683.
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):4001-4011. [Abstract]
- J Infect Dis. 2018 Nov 22;218(suppl_5):S365-S387. [Abstract]
- Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]
- Cancers (Basel). 2022 Nov 8;14(22):5481. [Abstract]
- Cancers. 2020 Jun 16;12(6):1596. [Abstract]
- Transl Oncol. 2024 Aug 16:49:102092. [Abstract]
- Sci Rep. 2022 Jul 20;12(1):12420. [Abstract]
- Sci Rep. 2021 Mar 8;11(1):5374. [Abstract]
- J Virol. 2023 Jun 29;97(6):e0037023. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Front Oncol. 2022 Apr 8;12:819003. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2023 Jul;396(7):1435-1450. [Abstract]
- J Pharm Biomed Anal. 2021 Apr 15:197:113933. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Jun 15;1147:122142. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2024 Aug 28;19(8):e0309289. [Abstract]
- PLoS One. 2022 Dec 22;17(12):e0279522. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Biomed Res Int. 2020 Jun 11;2020:9525207. [Abstract]
- Leuk Res. 2022 Sep:120:106920. [Abstract]
- Biomed Chromatogr. 2020 Mar;34(3):e4783. [Abstract]
- bioRxiv. 2026 Jun 25.
- bioRxiv. 2026 Apr 22:2026.04.19.719504. [Abstract]
- bioRxiv. 2026 Jan 25.
- Res Sq. 2025 Dec 18.
- bioRxiv. 2025 Nov 3:2025.11.02.685764. [Abstract]
- University of Innsbruck. 2025.
- bioRxiv. 2025 Sep 15.
- University of Jena. 2025.
- bioRxiv. 2025 February 23.
- Texas Southern University. 2024 July 02.
- bioRxiv. 2024 Nov 15:2024.11.11.623139. [Abstract]
- bioRxiv. 2023 Sep 16:2023.09.15.554413. [Abstract]
- Patent. US20220354911A1.
- Research Square Print. November 7th, 2022
- Department of Biochemistry. 2020 Oct.
Customer Validation & Images
-
In Vivo Efficacy Study
-
Cell Proliferation/Viability Assay
-
WB
-
WB
-
WB
Biologische Aktivität
|
CDK4 10 nM (IC50) |
CDK6 39 nM (IC50) |
Treating a panel of 17 neuroblastoma cell lines with Ribociclib (LEE011) across a four-log dose range (10 to 10,000 nM). Treatment with Ribociclib significantly inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Ribociclib treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition results in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 1374639-75-4
-
Appearance Solid
-
Molecular Weight 552.63
-
Formel C27H36N8O5
-
Color Light yellow to yellow
-
SMILES
O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5.OC(CCC(O)=O)=O
-
Synonyms
LEE011 succinate
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (84)
-
Journal Impact Factor
-
Most Recent
-
Cancer Cell
GABAergic neuronal lineage development determines clinically actionable targets in diffuse hemispheric glioma, H3G34-mutant. [Abstract]2024 Aug 27:S1535-6108(24)00305-2. PMID: 39232581 -
Cell
2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455 -
Cell
2023 Jun 8;186(12):2628-2643.e21. PMID: 37267950 -
Cancer Discov
INX-315, a selective CDK2 inhibitor, induces cell cycle arrest and senescence in solid tumors. [Abstract]2024 Mar 1;14(3):446-467. PMID: 38047585 -
Nat Cancer
Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. [Abstract]2021 Apr;2(4):429-443. PMID: 34568836 -
Mil Med Res
Expression dynamics of periodic transcripts during cancer cell cycle progression and their correlation with anticancer drug sensitivity. [Abstract]2022 Dec 19;9(1):71. PMID: 36529792 -
Cancer Res
Profiling the Activity of the Potent and Highly Selective CDK2 Inhibitor BLU-222 Reveals Determinants of Response in CCNE1-Aberrant Ovarian and Endometrial Tumors. [Abstract]2025 Apr 3;85(7):1297-1309. PMID: 39945650 -
Cancer Res
2019 Oct 15;79(20):5245-5259. PMID: 31395606 -
Mol Cell
2017 Oct 19;68(2):336-349.e6. PMID: 29053957 -
Nat Commun
Induced pluripotent stem cell-derived models of malignant nerve sheath tumor progression mimic glial to neuro-mesenchymal transition and uncover therapeutic opportunities. [Abstract]2026 Jun 17;17(1):5361. PMID: 42310314 -
Nat Commun
CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]2026 Jan 22;17(1):619. PMID: 41571637 -
Nat Commun
Targeting the Retinoblastoma/E2F repressive complex by CDK4/6 inhibitors amplifies oncolytic potency of an oncolytic adenovirus. [Abstract]2022 Aug 10;13(1):4689. PMID: 35948546 -
Nat Commun
Inhibition of CK1ε potentiates the therapeutic efficacy of CDK4/6 inhibitor in breast cancer. [Abstract]2021 Sep 10;12(1):5386. PMID: 34508104
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Sep 10;12(1):5386. [Abstract]
D4476 (150 mg/kg; i.g.; daily). Combination of D4476 with Ribociclib (100 mg/kg; i.g.; daily) retards MDA-MB-231 tumor growth in vivo.
-
Nat Commun
Co-targeting CDK4/6 and AKT with endocrine therapy prevents progression in CDK4/6 inhibitor and endocrine therapy-resistant breast cancer. [Abstract]2021 Aug 25;12(1):5112. PMID: 34433817
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
MPF-R and TPF-R cells were treated with different concentrations of the CDK4/6 inhibitor (CDK4/6i) Palbociclib (HY-A0065), Ribociclib (HY-15777C) or Abemaciclib (HY-16297A) for 6 days. Cell growth was measured by crystal violet colorimetric assay. Growth relative to vehicle (%) is plotted against log drug concentration.
-
Nat Commun
Death effector domain-containing protein induces vulnerability to cell cycle inhibition in triple-negative breast cancer. [Abstract]2019 Jun 28;10(1):2860. PMID: 31253784 -
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 -
Sci Adv
2022 Dec 23;8(51):eadc8911. PMID: 36563143 -
Cell Rep Med
CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]2025 Dec 29:102526. PMID: 41468895 -
Cell Rep Med
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity. [Abstract]2023 Oct 17;4(10):101200. PMID: 37734378 -
Clin Cancer Res
Triple Combination of MEK, BET, and CDK Inhibitors Significantly Reduces Human Malignant Peripheral Nerve Sheath Tumors in Mouse Models. [Abstract]2025 Mar 3;31(5):907-920. PMID: 39786423 -
Clin Cancer Res
CDK4 Amplification Reduces Sensitivity to CDK4/6 Inhibition in Fusion-Positive Rhabdomyosarcoma. [Abstract]2015 Nov 1;21(21):4947-59. PMID: 25810375
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]
Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2015 Nov 1;21(21):4947-59. [Abstract]
Retinoblastoma (RB) phosphorylation and FOXM1, another CDK4 target, are reduced in cells treated with LEE011.
-
Cancer Lett
A NIR-Ⅱ fluorescent probe for real-time visualization and early assessment of responses to CDK4/6 inhibitors in breast cancer. [Abstract]2026 May 28:646:218429. PMID: 41825845 -
Int J Biol Sci
Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. [Abstract]2019 Jan 1;15(3):522-532. PMID: 30745839 -
Cell Death Dis
2020 Sep 15;11(9):754. PMID: 32934219 -
Int J Biol Macromol
CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609. [Abstract]2024 Dec 27:139117. PMID: 39733900 -
NPJ Precis Oncol
Optimized culturing yields high success rates and preserves molecular heterogeneity, enabling personalized screening for high-grade gliomas. [Abstract]2025 May 27;9(1):156. PMID: 40425813 -
NPJ Precis Oncol
Acetylation of ELF5 suppresses breast cancer progression by promoting its degradation and targeting CCND1. [Abstract]2021 Mar 19;5(1):20. PMID: 33742100 -
NPJ Breast Cancer
CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]2025 Dec 3;11(1):135. PMID: 41339342 -
J Transl Med
Personalized medicine strategy for MPNSTs: using precision oncology on PDOX models to inform tumor boards. [Abstract]2026 Feb 4;24(1):385. PMID: 41639724 -
J Transl Med
CDK4/6 inhibitors sensitize gammaherpesvirus-infected tumor cells to T-cell killing by enhancing expression of immune surface molecules. [Abstract]2022 May 13;20(1):217. PMID: 35562811 -
Biomed Pharmacother
Ribociclib, a selective cyclin D kinase 4/6 inhibitor, inhibits proliferation and induces apoptosis of human cervical cancer in vitro and in vivo. [Abstract]2019 Apr:112:108602. PMID: 30784916 -
Cell Chem Biol
CDK2 heterobifunctional degraders co-degrade CDK2 and cyclin E resulting in efficacy in CCNE1-amplified and overexpressed cancers. [Abstract]2025 Apr 17;32(4):556-569.e24. PMID: 40250405 -
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 -
Eur J Cancer
Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ataxia telangiectasia-mutated kinase-mediated DNA damage response. [Abstract]2018 Oct:102:10-22. PMID: 30103095
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Eur J Cancer. 2018 Oct:102:10-22. [Abstract]
Head-to-head comparison of the effect of PD 0332991 and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.
-
Cell Rep
2020 Aug 4;32(5):107995. PMID: 32755587 -
Cell Rep
2017 Oct 31;21(5):1386-1398. PMID: 29091774 -
JCI Insight
RB expression confers sensitivity to CDK4/6 inhibitor-mediated radiosensitization across breast cancer subtypes. [Abstract]2022 Feb 8;7(3):e154402. PMID: 34932500 -
Int J Mol Med
2025 Nov;56(5):167. PMID: 40808344 -
Biochem Pharmacol
Direct reprogramming of human fibroblasts into hair-inducing dermal papilla cell-like cells by a single small molecule. [Abstract]2025 Jan 9:116744. PMID: 39798934 -
Breast Cancer Res
Estrogen receptor coregulator binding modulator (ERX-11) enhances the activity of CDK4/6 inhibitors against estrogen receptor-positive breast cancers. [Abstract]2019 Dec 26;21(1):150. PMID: 31878959 -
Pharmaceutics
A Dual-Payload Bispecific ADC Improved Potency and Efficacy over Single-Payload Bispecific ADCs. [Abstract]2025 Jul 25;17(8):967. PMID: 40870990 -
Mol Cancer Ther
Preclinical Activity of Abemaciclib Alone or in Combination with Antimitotic and Targeted Therapies in Breast Cancer. [Abstract]2018 May;17(5):897-907. PMID: 29483214 -
Cells
Machine Learning-Driven Multi-Omics Analysis Identifies CHP2 as a Key PANoptosis-Related Dual-Function Biomarker in Colorectal Cancer. [Abstract]2026 Feb 28;15(5):430. PMID: 41827864 -
Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
-
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Artif Cells Nanomed Biotechnol
Ribociclib (LEE011) suppresses cell proliferation and induces apoptosis of MDA-MB-231 by inhibiting CDK4/6-cyclin D-Rb-E2F pathway. [Abstract]2019 Dec;47(1):4001-4011. PMID: 31588803 -
J Infect Dis
2018 Nov 22;218(suppl_5):S365-S387. PMID: 30169850 -
Mol Oncol
Palbociclib induces activation of AMPK and inhibits hepatocellular carcinoma in a CDK4/6-independent manner. [Abstract]2017 Aug;11(8):1035-1049. PMID: 28453226
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]
Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.
Ribociclib succinate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]
Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM for 72 h.
-
Cancers (Basel)
Combined Targeting of Pathogenetic Mechanisms in Pancreatic Neuroendocrine Tumors Elicits Synergistic Antitumor Effects. [Abstract]2022 Nov 8;14(22):5481. PMID: 36428573 -
Cancers
Targeting Pharmacokinetic Drug Resistance in Acute Myeloid Leukemia Cells with CDK4/6 Inhibitors. [Abstract]2020 Jun 16;12(6):1596. PMID: 32560251 -
Transl Oncol
Radiosensitizing effects of CDK4/6 inhibitors in hormone receptor-positive and HER2-negative breast cancer mediated downregulation of DNA repair mechanism and NF-κB-signaling pathway. [Abstract]2024 Aug 16:49:102092. PMID: 39153367 -
Sci Rep
2022 Jul 20;12(1):12420. PMID: 35859155 -
Sci Rep
2021 Mar 8;11(1):5374. PMID: 33686114 -
J Virol
2023 Jun 29;97(6):e0037023. PMID: 37219458 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Front Oncol
CDK6 Immunophenotype Implicates Potential Therapeutic Application of CDK4/6 Inhibitors in Urothelial Carcinoma. [Abstract]2022 Apr 8;12:819003. PMID: 35463324 -
Naunyn Schmiedebergs Arch Pharmacol
Piperazine ring toxicity in three novel anti-breast cancer drugs: an in silico and in vitro metabolic bioactivation approach using olaparib as a case study. [Abstract]2023 Jul;396(7):1435-1450. PMID: 36738368 -
J Pharm Biomed Anal
Identification and structural characterization of potential degraded impurities of ribociclib by time of flight -tandem mass spectrometry, and their toxicity prediction. [Abstract]2021 Apr 15:197:113933. PMID: 33588298 -
J Chromatogr B Analyt Technol Biomed Life Sci
Time of flight mass spectrometry based in vitro and in vivo metabolite profiling of ribociclib and their toxicity prediction. [Abstract]2020 Jun 15;1147:122142. PMID: 32416594 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
The effect of ribociclib on the expression levels of miR-141 and CDK4/6-USP51 signaling pathway genes in MCF-7 and MDA-MB-231 cells. [Abstract]2024 Aug 28;19(8):e0309289. PMID: 39196911 -
PLoS One
Combination of androgen receptor inhibitor enzalutamide with the CDK4/6 inhibitor ribociclib in triple negative breast cancer cells. [Abstract]2022 Dec 22;17(12):e0279522. PMID: 36548336 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Biomed Res Int
Inhibition of the CDK4/6-Cyclin D-Rb Pathway by Ribociclib Augments Chemotherapy and Immunotherapy in Renal Cell Carcinoma. [Abstract]2020 Jun 11;2020:9525207. PMID: 32626773 -
Leuk Res
Targeting cyclin-dependent kinases 4/6 inhibits survival of megakaryoblasts in acute megakaryoblastic leukaemia. [Abstract]2022 Sep:120:106920. PMID: 35872339 -
Biomed Chromatogr
Metabolic profiles of ribociclib in rat and human liver microsomes using liquid chromatography combined with electrospray ionization high-resolution mass spectrometry. [Abstract]2020 Mar;34(3):e4783. PMID: 31899811 -
-
bioRxiv
CDK4/6 inhibition sensitizes breast cancer to NK cell therapy by inducing immune-interactive surface proteins. [Abstract]2026 Apr 22:2026.04.19.719504. PMID: 42079201 -
-
-
bioRxiv
2025 Nov 3:2025.11.02.685764. PMID: 41279360 -
-
-
-
-
-
bioRxiv
Therapeutic benefits of maintaining CDK4/6 inhibitors and incorporating CDK2 inhibitors beyond progression in breast cancer. [Abstract]2024 Nov 15:2024.11.11.623139. PMID: 39605351 -
bioRxiv
CDK6-mediated endothelial cell cycle acceleration drives arteriovenous malformations in hereditary hemorrhagic telangiectasia. [Abstract]2023 Sep 16:2023.09.15.554413. PMID: 37745444 -
-
-
Lösungsmittel & Löslichkeit
DMSO : 9.38 mg/mL (16.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4.17 mg/mL (7.55 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 0.94 mg/mL (1.70 mM); Clear solution
This protocol yields a clear solution of ≥ 0.94 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.4 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: ≥ 0.94 mg/mL (1.70 mM); Clear solution
This protocol yields a clear solution of ≥ 0.94 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.4 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 3.12 mg/mL (5.65 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 15.15 mg/mL (27.41 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Cells are grown for 24 hours in 35 mm plates, treated with 500 nM Ribociclib for 6 days, and then fixed and stained overnight. Cells are then imaged for SA-β-gal using an Axio Observer D.1 phase contrast microscope. The percentage of SA-β-gal positive cells is determined by counting the number of positive cells present in three separate microscope frames, and then normalizing to the control. To assess apoptotic activity, cells are plated in triplicate in 96 well plates, treated with Ribociclib, and assayed for caspase 3/7 activation 16 hours after treatment with Caspase-Glo 3/7. Cells treated with SN-38 are used as a positive control[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
The BE2C, NB-1643, or EBC1 cell line-derived xenografts are implanted subcutaneously into the right flank of CB17 SCID-/- mice. Animals bearing engrafted tumors of 200-600 mm3 are then randomized to oral treatment with 200 mg/kg Ribociclib in 0.5 % methylcellulose (n=10) or vehicle (n=10) daily for a total of 21 days. Tumor burden is determined periodically throughout treatment according to the formula (π/6)×d2, where d represents the mean tumor diameter obtained by caliper measurement.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (280 KB)
-
SDS (788 KB)
- English - EN (788 KB)
- Français - FR (788 KB)
- Deutsch - DE (788 KB)
- Norwegian - NO (788 KB)
- Español - ES (788 KB)
- Swedish - SV (788 KB)
- Italian - IT (788 KB)
- Korean - KR (788 KB)
- Portuguese - PT (788 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10. [Content Brief]
[2]. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.8095 mL | 9.0476 mL | 18.0953 mL | 45.2382 mL |
| 5 mM | 0.3619 mL | 1.8095 mL | 3.6191 mL | 9.0476 mL | |
| DMSO | 10 mM | 0.1810 mL | 0.9048 mL | 1.8095 mL | 4.5238 mL |
| 15 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0159 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.
Ribociclib succinate Related Classifications
HY-15777B Related Classifications
Powered by Bioz