All AbMole products are for research use only, cannot be used for human consumption.
LY2835219 mesylate is a potent and selective CDK4/6 dual inhibitor with potential antineoplastic activity. CDK4/6 dual inhibitor LY2835219 has been shown in vitro to be a selective ATP-competitive inhibitor of CDK4/6 that inhibits phosphorylation of the Rb tumor suppressor protein and thereby induces G1 cell cycle arrest. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. LY2835219 is being investigated in a phase I clinical trial and in a clinical trial for the treatment of mantle cell lymphoma.
JCI Insight. 2022 Sep 8;7(17):e151851.
Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition
LY2835219 mesylate purchased from AbMole
Cancer Cell. 2018 Sep 10;34(3):411-426.e19.
Identification of Therapeutic Targets in Rhabdomyosarcoma through Integrated Genomic, Epigenomic, and Proteomic Analyses.
LY2835219 mesylate purchased from AbMole
Sci Rep. 2018 Nov 8;8(1):16579.
Different responses of colorectal cancer cells to alternative sequences of cetuximab and oxaliplatin.
LY2835219 mesylate purchased from AbMole
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Source | Cancer Cell (2018). Figure 5. abemaciclib (Abmole Bioscience, Houston, USA) |
| Method | oral gavage | |
| Cell Lines | Mice | |
| Concentrations | 50 mg/kg | |
| Incubation Time | — | |
| Results | Mice treated with IRN + VCR had stable disease (SD), whereas mice treated with either palbociclib + trametinib or abemaciclib + trametinib exhibited progressive disease. |
 |
Source | Invest New Drugs (2014). Figure 2. LY2835219 |
| Method | flow cytometry | |
| Cell Lines | MCF10A cells | |
| Concentrations | 5 μM | |
| Incubation Time | 24-hour | |
| Results | LY2835219 induced a G1 arrest in Rb-proficient MDA-MB-231 breast cancer cells, whereas no such effect was seen in Rb-deficient MDA-MB-468 breast cancer cells at compound concentrations up to 2,500 nmol/L |
| Molecular Weight | 602.7 |
| Formula | C27H32F2N8.CH4O3S |
| CAS Number | 1231930-82-7 |
| Solubility (25°C) | Water 90 mg/mL DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| R547
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| JNJ-7706621
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| PD 0332991 HCL
PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. |
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