Abemaciclib (LY2835219) mesylate

Alias: Abemaciclib; LY-2835219 mesylate; LY2835219; LY 2835219; Abemaciclib mesylate
Cat No.:V1547 Purity: =99.48%
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.
Abemaciclib (LY2835219) mesylate Chemical Structure CAS No.: 1231930-82-7
Product category: CDK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
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Other Forms of Abemaciclib (LY2835219) mesylate:

  • Abemaciclib (LY2835219)
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Abemaciclib (LY2835219) mesylate has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Purity: =99.48%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
CDK4 (IC50 = 2 nM); CDK6 (IC50 = 10 nM)
ln Vitro

LY2835219 is a cyclin-dependent kinase (CDK) inhibitor that can be taken orally and has the ability to inhibit cancer by targeting the cell cycle pathways of CDK4 (cyclin D1) and CDK6 (cyclin D3). LY2835219 selectively inhibits CDK4 and 6, which prevents the phosphorylation of the retinoblastoma (Rb) protein during the early stages of growth. Rb phosphorylation inhibition stops CDK-mediated G1-S phase transition, which stops the cell cycle in the G1 phase, inhibits DNA synthesis, and stops the growth of cancer cells. Cell cycle disruption is brought on by the overexpression of the serine/threonine kinases CDK4/6, which is observed in some cancer types.[1]

ln Vivo
LY2835219 has an unbound plasma IC50 of approximately 95 nM, which saturates BBB efflux. The percentage of LY2835219-MsOH dose in the brain ranges from 0.5-2.9%. LY2835219-MsOH, when used alone or in conjunction with temozolomide, inhibited tumor growth in a dose-dependent manner in both a subcutaneous and intracranial human glioblastoma model (U87MG).[1]
Animal Protocol
Female C57BL/6 mice
50 mg/kg
i.p.
References

[1]. Drug Des Devel Ther . 2018 Feb 16:12:321-330.

[2]. Nat Med . 2021 Feb;27(2):289-300.

[3]. Theranostics . 2020 Aug 25;10(23):10619-10633.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H36F2N8O3S
Molecular Weight
602.7
Exact Mass
602.26
Elemental Analysis
C, 55.80; H, 6.02; F, 6.30; N, 18.59; O, 7.96; S, 5.32
CAS #
1231930-82-7
Appearance
Solid powder
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
InChi Key
NCJPFQPEVDHJAZ-UHFFFAOYSA-N
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)
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
Synonyms
Abemaciclib; LY-2835219 mesylate; LY2835219; LY 2835219; Abemaciclib mesylate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~83 mg/mL (~137.7 mM)
Water: ~100 mg/mL (~165.9 mM)
Ethanol: ~24 mg/mL (~39.8 mM)
Solubility (In Vivo)
Water: 100 mg/mL (~165.9 mM)
 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Abemaciclib (LY2835219)


    Effects of LY2835219 on RB pathway and intracellular signaling.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Combined effect of LY2835219 and mTOR inhibitorsin vitro.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    LY2835219 and mTOR inhibitor combination in HNSCC xenograft tumor model.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Antitumor activity of LY2835219 in HNSCC xenograft tumor model.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Effects of CDK4/6 inhibitor LY2835219 on cell growth in HNSCC.2016 Mar 22;7(12):14803-13.

  • Abemaciclib (LY2835219)


    Effects of LY2835219 on cell proliferation and cell cycle in HNSCC.2016 Mar 22;7(12):14803-13.

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