Formaat : 5mg
Telefoonnummer : +1 850 650 7790
Synonyms: LY2835219, CDK4/6 dual inhibitor
| Description | Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer. |
| Targets & IC50 | CDK1:1627 nM, CDK1-cyclinB1:1627 nM, CDK5:355 nM, CDK5-p35:287 nM, CDK7-CyclinH-MAT1:3910 nM, FLT3 (D835Y):403 nM, DYRK2:61 nM, DRAK1:659 nM, CDK2:504 nM, GSK3b:192 nM, CK2:117 nM, JNK3:389 nM, GSK-3β:192 nM, CDK2-CyclinE:504 nM, PIM2:3400 nM, CDK7:3910 nM, CDK4:2 nM, CDK9-CyclinT1:57 nM, PIM1:50 nM, CDK6:10 nM, HIPK2:31 nM, FLT3:3960 nM, CDK5-p25:355 nM |
| In vitro | METHODS: HNSCC cell lines OSC-19, FaDu and YD-10B were treated with Abemaciclib (0.01-10 μM) for 72 h, and cell viability was measured by Cell Counting Kit. RESULTS: Abemaciclib treatment decreased the cell viability of HNSCC cells with IC50 values ranging from 0.5 μM to 0.7 μM. [1] METHODS: AML cells MV4-11 were treated with Abemaciclib (0.04-5 μM) for 24 h. The cell cycle was detected using Flow Cytometry. RESULTS: Abemaciclib induced G1 phase block in MV4-11 cells. The G1-phase block was maximized when the concentration was ≥320 nmol/L. The RESULTS showed that Abemaciclib induced G1-phase block in MV4-11 cells. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, Abemaciclib (45-90 mg/kg in 1% HEC in 20 mM phosphate buffer (pH 2.0)) was administered by gavage to BALB/c mice bearing human tongue squamous carcinoma tumors OSC-19 once daily for fourteen days. RESULTS: Abemaciclib significantly reduced tumor growth in OSC-19 xenografts during treatment. abemaciclib treatment decreased AKT phosphorylation but had no effect on mTOR activation. [1] METHODS: To assay antitumor activity in vivo, Abemaciclib (22.5-90 mg/kg in 1% HEC in 25 mmol/L PB pH2) was administered by gavage to athymic nude mice harboring melanoma A375 once a day for twenty-one days. RESULTS: Statistically significant tumor growth inhibition was observed with Abemaciclib at 45 or 90 mg/kg dosing regimens. abemaciclib treatment significantly reduced pS780-Rb and pS10-Histone H3 levels, suggesting that CDK4/6 inhibition resulted in cell cycle inhibition and reduced tumor cell proliferation. [3] |
| Synonyms | LY2835219, CDK4/6 dual inhibitor |
| Kinase Assay | Cells (5×103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader. |
| Cell Research | LY2835219 is dissolved in DMSO to a 10 mM concentration.? Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of <1 is synergistic and a CI of >1 is antagonistic. |
| Molecular Weight | 506.59 |
| Formula | C27H32F2N8 |
| Cas No. | 1231929-97-7 |
| Smiles | C(C)(C)N1C=2C(=C(F)C=C(C2)C3=NC(NC4=CC=C(CN5CCN(CC)CC5)C=N4)=NC=C3F)N=C1C |
| Relative Density. | 1.32 g/cm3 (Predicted) |
| Storage | Keep away from direct sunlight, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: < 1 mg/mL (insoluble or slightly soluble), Sonication is recommended.  Ethanol: 1.69 mg/mL (3.34 mM), Sonication is recommended. | ||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 0.1 mg/mL (0.2 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||
Solution Preparation Table | |||||||||||
Ethanol
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
