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. |
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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
| Q901
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