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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Abemaciclib mesylate (formerly known as LY-2835219; LY2835219; trade name: Verzenio) is a potent and selective, orally bioavailable dual inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with potential antineoplastic activity. In assays without cells, it inhibits CDK4/6 with IC50 values of 2 nM and 10 nM, respectively. Abemaciclib received FDA approval in September 2017 to treat specific advanced or metastatic breast cancers. In early G1, retinoblastoma (Rb) protein phosphorylation is inhibited by LY2835219 through selective inhibition of CDK4 and 6. By stopping CDK-mediated G1-S phase transition, inhibition of Rb phosphorylation stops the cell cycle in the G1 phase, inhibiting DNA synthesis and slowing the growth of cancer cells. As observed in some cancer forms, overexpression of the serine/threonine kinases CDK4/6 can result in cell cycle dysregulation.
Targets |
CDK4 (IC50 = 2 nM); CDK6 (IC50 = 10 nM)
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ln Vitro |
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ln Vivo |
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Animal Protocol |
Female C57BL/6 mice
50 mg/kg i.p. |
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References |
Molecular Formula |
C28H36F2N8O3S
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Molecular Weight |
602.7
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Exact Mass |
602.26
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Elemental Analysis |
C, 55.80; H, 6.02; F, 6.30; N, 18.59; O, 7.96; S, 5.32
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CAS # |
1231930-82-7
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Related CAS # |
Abemaciclib;1231929-97-7
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Appearance |
Solid powder
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SMILES |
CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F.CS(=O)(=O)O
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InChi Key |
NCJPFQPEVDHJAZ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H32F2N8.CH4O3S/c1-5-35-8-10-36(11-9-35)16-19-6-7-24(30-14-19)33-27-31-15-22(29)25(34-27)20-12-21(28)26-23(13-20)37(17(2)3)18(4)32-26;1-5(2,3)4/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34);1H3,(H,2,3,4)
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Chemical Name |
N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine;methanesulfonic acid
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Synonyms |
Abemaciclib; LY-2835219 mesylate; LY2835219; LY 2835219; Abemaciclib mesylate
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (3.32 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2 mg/mL (3.32 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: Water: 100 mg/mL (~165.9 mM) Solubility in Formulation 7: 25 mg/mL (41.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 8: 12.5 mg/mL (20.74 mM) in 0.5% HEC (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6592 mL | 8.2960 mL | 16.5920 mL | |
5 mM | 0.3318 mL | 1.6592 mL | 3.3184 mL | |
10 mM | 0.1659 mL | 0.8296 mL | 1.6592 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effects of LY2835219 on RB pathway and intracellular signaling.Oncotarget.2016 Mar 22;7(12):14803-13. th> |
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Combined effect of LY2835219 and mTOR inhibitorsin vitro.Oncotarget.2016 Mar 22;7(12):14803-13. td> |
LY2835219 and mTOR inhibitor combination in HNSCC xenograft tumor model.Oncotarget.2016 Mar 22;7(12):14803-13. td> |
Antitumor activity of LY2835219 in HNSCC xenograft tumor model.Oncotarget.2016 Mar 22;7(12):14803-13. th> |
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Effects of CDK4/6 inhibitor LY2835219 on cell growth in HNSCC.Oncotarget.2016 Mar 22;7(12):14803-13. td> |
Effects of LY2835219 on cell proliferation and cell cycle in HNSCC.Oncotarget.2016 Mar 22;7(12):14803-13. td> |